潘托拉唑钠原料药，潘托拉唑钠厂家，潘托拉唑钠价格
您当前的位置： &
& 潘托拉唑钠原料药，潘托拉唑钠厂家，潘托拉唑钠价格
点击图片查看大图
潘托拉唑钠原料药，潘托拉唑钠厂家，潘托拉唑钠价格&
1.00元/千克&
最小起订量：
供货总量：
发货期限：
自买家付款之日起 3 天内发货
发布时间：
17:38:25&&有效期至：长期有效
更新时间：
&李经理 &&：027- &&&&&&&QQ:
公司名称：湖北康宝泰精细化工有限公司
潘托拉唑钠
潘托拉唑钠中文名称：潘托拉唑钠
潘托拉唑钠英文名称：Pantoprazole Sodium
潘托拉唑钠中文别名：泮托拉唑钠;5-二氟甲氧基-2-[(3,4-二甲氧基-2-吡啶基)甲基]亚硫酰基-1H-苯骈咪唑钠盐
潘托拉唑钠物理性质及其指标
潘托拉唑钠性状:白色或类白色结晶粉末
潘托拉唑钠CAS：-1
潘托拉唑钠分子式：C16H14F2N3NaO4S
潘托拉唑钠分子量：405.3516
潘托拉唑钠EINECS号：
潘托拉唑钠
C16H14F2N3NaO4S
Pantoprazole Sodium
潘托拉唑钠含量：标准为99以上
潘托拉唑钠用途：抗酸药及抗溃疡药，用于治疗胃及十二指肠溃疡病.适用于十二指肠溃疡、胃溃疡急性胃粘膜病变，复合性胃溃疡等急性上消化道出血的治疗。
潘托拉唑钠关于运费：我公司无特殊说明外，所有报价均由我公司承担运费。潘托拉唑钠关于货期。无特殊情况说明，我公司均为现货。潘托拉唑钠的溶解性，潘托拉唑钠的价格，潘托拉唑钠在水中的溶解性，兰索拉唑在生理盐水中的溶解性;潘托拉唑钠的质量标准，潘托拉唑钠的分析方法。以上相关信息请直接联系湖北康宝泰精细化工有限公司，我司将随货提供部分的参考信息。
李经理 &&：027- &&&&&&&QQ:
客户您的满意是我们的追求，优惠的价格和良好的售后服务是我们企业得以长期发展的灵魂！！
我公司长期销售多种原料药和中间体，欢迎新老顾客前来选购！本产品网址：/b2b/hbkbtjxhg/sell/itemid-.html处方药西药医保乙类进口批准文号：H21063102生产企业：功能主治：十二指肠溃疡
中、重度反流性食管炎与下述药物配伍用能够根除幽门螺杆菌感染：
克拉霉素和阿莫西林，或克拉霉素和甲硝唑，或阿莫西林和甲硝唑(详见用药方法)以减少该微生物感染所致的十二指肠溃疡与胃溃疡的复发。
泮托拉唑不用于治疗病变轻微的胃肠道疾患，如神经性消化不良。
在应用泮托拉唑治疗胃溃疡前，须除外胃与食道的恶性病变，以免因症状缓解而延误诊断。
反流性食管炎的诊断应经内镜检查核实。用法用量：本品若无医师特殊处方，应按下述方法服用，请遵守这些方法，否则可能疗效不佳。
对伴有幽门螺杆菌感染的十二指肠溃疡或胃溃疡须用联合疗法根除感染。泮托拉唑与抗菌药物的联合使用可采取下述任何一种方案：
a. 1片泮托拉唑肠溶片×2次/日 + 1000 mg 阿莫西林 × 2次/日 + 500 mg 克拉霉素×2次/日
b. 1片泮托拉唑肠溶片×2次/日 + 500 mg甲硝唑×2次/日 + 500 mg克拉霉素×2次/日
c. 1片泮托拉唑肠溶片×2次/日 + 1000 mg阿莫西林×2次/日 + 500 mg甲硝唑×2次/日
在联合疗法中，有甲硝唑的方案仅在其他方案不能根除幽门螺杆菌感染的情况下方予使用。
若患者无联合疗法的指征，如检查幽门螺杆菌阴性，泮托拉唑可按下述剂量单独使用，除非另有医师处方：
十二指肠溃疡、胃溃疡和反流性食管炎患者一般每日服用1片泮托拉唑肠溶片。个别病例，特别是在其它治疗方法无效的情况下，可将剂量加倍(即每日2片泮托拉唑肠溶片)。
肾功能受损和老年患者每日泮托拉唑的剂量一般不应超过40mg，但有些情况例外，即为根除幽门螺杆菌感染而使用联合疗法时，老年患者在1周治疗中也使用常规剂量(40mg ×2/日)的泮托拉唑。
严重肝功能受损的患者剂量应减少至隔日1片(40mg泮托拉唑肠溶片)。
服药方式与疗程
本品不能咀嚼或咬碎，应在早餐前1小时配水完整服用。为根除幽门螺杆菌感染而使用联合疗法时，每日第2次服药应在晚餐前进行。联合疗法一般持续7天，此后如症状持续存在，需继续服用泮托拉唑以保证溃疡的完全愈合，用药应遵守治疗胃、十二指肠溃疡的推荐剂量。
通常十二指肠溃疡在2周内愈合，如果2周的疗程不够，可继续延长治疗2周。
胃溃疡和反流性食管炎需要治疗4周。如果疗程不够，可继续延长治疗4周。
由于长期用药的经验有限，疗程不宜超过8周。相关疾病：￥87.8起请仔细阅读潘妥洛克说明书并按说明使用或在医师指导下购买和使用￥87.8起八百方医药健康网购商城￥321健客网网上药店￥370潘妥洛克说明书通用名称：泮托拉唑肠溶片功能主治：十二指肠溃疡
中、重度反流性食管炎与下述药物配伍用能够根除幽门螺杆菌感染：
克拉霉素和阿莫西林，或克拉霉素和甲硝唑，或阿莫西林和甲硝唑(详见用药方法)以减少该微生物感染所致的十二指肠溃疡与胃溃疡的复发。
泮托拉唑不用于治疗病变轻微的胃肠道疾患，如神经性消化不良。
在应用泮托拉唑治疗胃溃疡前，须除外胃与食道的恶性病变，以免因症状缓解而延误诊断。
反流性食管炎的诊断应经内镜检查核实。用法用量：本品若无医师特殊处方，应按下述方法服用，请遵守这些方法，否则可能疗效不佳。
对伴有幽门螺杆菌感染的十二指肠溃疡或胃溃疡须用联合疗法根除感染。泮托拉唑与抗菌药物的联合使用可采取下述任何一种方案：
a. 1片泮托拉唑肠溶片×2次/日 + 1000 mg 阿莫西林 × 2次/日 + 500 mg 克拉霉素×2次/日
b. 1片泮托拉唑肠溶片×2次/日 + 500 mg甲硝唑×2次/日 + 500 mg克拉霉素×2次/日
c. 1片泮托拉唑肠溶片×2次/日 + 1000 mg阿莫西林×2次/日 + 500 mg甲硝唑×2次/日
在联合疗法中，有甲硝唑的方案仅在其他方案不能根除幽门螺杆菌感染的情况下方予使用。
若患者无联合疗法的指征，如检查幽门螺杆菌阴性，泮托拉唑可按下述剂量单独使用，除非另有医师处方：
十二指肠溃疡、胃溃疡和反流性食管炎患者一般每日服用1片泮托拉唑肠溶片。个别病例，特别是在其它治疗方法无效的情况下，可将剂量加倍(即每日2片泮托拉唑肠溶片)。
肾功能受损和老年患者每日泮托拉唑的剂量一般不应超过40mg，但有些情况例外，即为根除幽门螺杆菌感染而使用联合疗法时，老年患者在1周治疗中也使用常规剂量(40mg ×2/日)的泮托拉唑。
严重肝功能受损的患者剂量应减少至隔日1片(40mg泮托拉唑肠溶片)。
服药方式与疗程
本品不能咀嚼或咬碎，应在早餐前1小时配水完整服用。为根除幽门螺杆菌感染而使用联合疗法时，每日第2次服药应在晚餐前进行。联合疗法一般持续7天，此后如症状持续存在，需继续服用泮托拉唑以保证溃疡的完全愈合，用药应遵守治疗胃、十二指肠溃疡的推荐剂量。
通常十二指肠溃疡在2周内愈合，如果2周的疗程不够，可继续延长治疗2周。
胃溃疡和反流性食管炎需要治疗4周。如果疗程不够，可继续延长治疗4周。
由于长期用药的经验有限，疗程不宜超过8周。剂型：片剂 不良反应：1.消化系统
上腹痛、腹泻、便秘或腹胀
2.神经系统
头痛本品不能用于已知对该药的某种成分过敏的患者。
在根除幽门螺杆菌感染的联合疗法中，有中、重度肝肾功能障碍的患者禁用本品，因为目前尚缺乏联合疗法对这类患者疗效及安全性的临床经验。当与其他药物联合使用时，每种药物的用药原则均应予以遵守。遇有严重肝功能障碍(肝衰竭)的患者，应定期监测肝脏酶谱的变化，若其测定值增加，必须停止用药。
不要使用过期的泮托拉唑。
药品应存放在儿童接触不到的地方。本品主要成份为：泮托拉唑(Pantoprazole)倍半水合钠盐。本品为黄色肠溶衣片，除去包衣后显白色或类白色。对孕妇的临床经验有限。动物试验中，在剂量超过5mg/kg时有轻度胚胎毒性作用。无泮托拉唑进入人体乳汁的报道。只有当泮托拉唑对母体的益处大于其对胎儿或婴儿的潜在危害时，才可使用本品。目前还没有将之用于儿童的经验。参见【用法用量】的注意项。本品可能减少生物利用度取决于胃内PH值的药物(如酮康唑)的吸收。请注意，这也适用于口服本品之前的短暂时间内所应用的药物。
泮托拉唑的活性成分在肝脏内通过细胞色素P450酶系代谢， 因此凡通过该酶系代谢的其它药物均不能除外与之有相互作用的可能性。然而对许多这类药物进行专门检测，如卡马西平、咖啡因、安定、双氯芬酸、地高辛、乙醇、格列本脲、美托洛尔、萘普生、硝苯地平、苯丙香豆素、苯妥英、吡罗昔康、茶碱、华法林和口服避孕药等，却未观察到泮托拉唑与之有明显临床意义的相互作用。
泮托拉唑与同时使用的抗酸药也没有相互作用。泮托拉唑是苯并咪唑衍生物，通过特异性地与胃壁细胞上的质子泵结合，抑制胃酸分泌。
泮托拉唑在胃壁细胞的酸性分泌小管中被激活，再特异性地与胃酸分泌的最终环节－质子泵（即H+，K+-ATP酶）结合，抑制胃酸分泌。 抑酸效应呈剂量相关性，能够有效抑制基础、夜间胃酸分泌。与其他质子泵抑制剂和H2受体拮抗剂一样，泮托拉唑可降低胃酸分泌，刺激胃泌素水平相应升高，这种效应是可逆的。本品能够有效抑制基础、夜间及24小时胃酸分泌，抑酸效应呈现出剂量相关性。
本品药代动力学呈线性特征，静脉输入或口服10-80 mg后，AUC（ 浓度时间曲线下面积）和Cmax（血药浓度峰值）均随剂量的增加而成比例上升。其表观分布容积为 0.15 L/kg ， 清除率为0.1L/h/kg， 清除半衰期( t1/2 )约为1小时，血浆蛋白结合率为98％。
药物代谢 本品几乎均在肝脏内经细胞色素P450酶系代谢， 并另有II期代谢的途径。主要代谢物为泮托拉唑去甲基硫酸酯，其大部分（约80％）由肾脏排出，其余由胆汁分泌从粪便中排出。潘妥洛克咨询评价用前咨询用后评价全国药店位置筛选：江西全部极速送药潘妥洛克生产企业：Takeda GmbH production site Oranienburg温馨提示：请留下您的信息，我们会尽快与您联系价
格：87.8起包装选择：40mg*7片/盒40mg*14片/盒数
名：请输入正确的姓名手
机：请输入正确的手机号，方便商家与您联系验证码：获取验证码请输入正确的验证码位
置：北京北京区/县东城区西城区海淀区朝阳区崇文区宣武区丰台区石景山区房山区门头沟区通州区顺义区昌平区怀柔区平谷区大兴区密云县延庆县请选择您的地区地
址：填写更详细的地址，仅支持汉字、字母、数字、-#备
注：仅支持汉字、字母、数字、-#，最多可填写300个字符提示：商品均来自正规合法药房，您成功提交后，专业药师会根据审核结果主动与您联系。急速送药提交失败信息提交失败，请关闭重新填写秒钟后该页面自动返回急速送药提交成功已成功提交，10分钟内给您回复。秒钟后该页面自动返回温馨提示：晚上6点后提交的需求将在次日早上10点前回复& Pantoprazole sodium, DZ-2352a, B-8510-29(free acid), By-1023
Pantoprazole sodium, DZ-2352a, B-8510-29(free acid), By-1023
摘 要：Pantoprazole sodium, DZ-2352a, B-8510-29(free acid), By-1023/SK&F-96022(free acid), B-8610-23/SK&F-96022-Z, Pantorc, Rifun, Pantozol, Zurcal, Ulcotenal, Inipomp, Pantecta, Anagastra, Pantoloc, Pantopan, Inipomp, Peptazol, Protonix, Protium,-
【药物名称】Pantoprazole sodium, DZ-2352a, B-8510-29(free acid), By-1023/SK&F-96022(free acid), B-8610-23/SK&F-96022-Z, Pantorc, Rifun, Pantozol, Zurcal, Ulcotenal, Inipomp, Pantecta, Anagastra, Pantoloc, Pantopan, Inipomp, Peptazol, Protonix, Protium
【化学名】5-(Difluoromethoxy)-2-(3,4-dimethoxypyridin-2-ylmethylsulfinyl)-1H-benzimidazole sodium salt
【CAS登记号】-1, -7 (free acid), -2 (sesquihydrate)
【结构式】
【分子式】C16-H14-F2-N3-O4-S.Na
【分子量】405.358
【原研厂家】Altana Pharma (Originator), Recordati (Not Determined), Abbott (Licensee), Daiichi Pharmaceutical (Licensee), Madaus (Licensee), Nycomed Pharma (Licensee), Pfizer (Licensee), Ravizza (Licensee), Roche (Licensee), Sanofi-Synthlabo (Licensee), Schwarz (Lic
【作用类别】Anti-Helicobacter Pylori Agents, Antiulcer Drugs, Esophageal Diseases, Treatment of, Gastric Antisecretory Drugs, Gastroesophageal Reflux Disease, Agents for, GASTROINTESTINAL DRUGS, H+/K+-ATPase Inhibitors
【研发状态】Launched-1994
【合成情况】　
〖来源〗J Label Compd Radiopharm
〖合成路线〗
〖标题〗The synthesis of [14C]pantoprazole - SK&F 96022Z - An H+/K+ ATP inhibitor
〖合成方法〗A new synthesis of [14C]-labeled pantoprazole has been described:
The cyclization of potassium [14C]-ethylxanthate (I) with the diaminobenzene (II) by means of NaOH gives the imidazole (III), which is condensed with 2-(chloromethyl)-3,4-dimethoxypyridine (IV) by means of NaOH in ethanol to afford the sulfide (V). Finally, this compound is oxidized with m-chloroperbenzoic acid (mcpba) in dichloromethane.
〖作者〗Saunders, D.; Lawrie, K.W.M.; Crowe, A.M.; Johnston, C.E.A.
〖参考〗Saunders, D.; Lawrie, K.W.M.; Crowe, A.M.; Johnston, C.E.A.; The synthesis of [14C]pantoprazole - SK&F 96022Z - An H+/K+ ATP inhibitor. J Label Compd Radiopharm , 409
〖出处〗J Label Compd Radiopharm):409
〖备注〗A new synthesis of [14C]-labeled pantoprazole has been described:
1) The cyclization of potassium [14C]-ethylxanthate (I) with the diaminobenzene (II) by means of NaOH gives the imidazole (III), which is condensed with 2-(chloromethyl)-3,4-dimethoxypyridine (IV) by means of NaOH in ethanol to afford the sulfide (V). Finally this compound is oxidized with m-chloroperbenzoic acid (mcpba) in dichloromethane (Scheme a).
2) Using [14C]-labeled (IV)in the preceding synthesis, pantoprazole labeled in the methylene was obtained. Intermediate (IV) labeled in the methylene attached to the pyridine ring can be prepared as follows:
The reaction of 2-bromo-3,4-dimethoxypyridine (V) with [14C]-labeled CuCN gives 3,4-dimethoxypyridine-2-carbonitrile (VI), which is hydrolyzed with NaOH and methylated with diazomethane to the methyl ester (VII). Finally this compound is reduced with LiAlH4 to the corresponding alcohol and treated with SOCl2 to give the chloromethylpyridine (IV*) with the [14C] label. Then this compound is condensed with benzimidazole (III) as usual.(Scheme a).
〖来源〗J Label Compd Radiopharm
〖合成路线〗
〖标题〗The synthesis of [14C]pantoprazole - SK&F 96022Z - An H+/K+ ATP inhibitor
〖合成方法〗Using [14C]-labeled (IV) in the preceding synthesis, pantoprazole labeled in the methylene was obtained. Intermediate (IV) labeled in the methylene attached to the pyridine ring can be prepared as follows:
The reaction of 2-bromo-3,4-dimethoxypyridine (V) with [14C]-labeled CuCN gives 3,4-dimethoxypyridine-2-carbonitrile (VI), which is hydrolyzed with NaOH and methylated with diazomethane to the methyl ester (VII). Finally, this compound is reduced with LiAlH4 to the corresponding alcohol and treated with SOCl2 to give the chloromethylpyridine (IV*) with the [14C] label. Then this compound is condensed with benzimidazole (III) as usual.
〖作者〗Saunders, D.; Lawrie, K.W.M.; Crowe, A.M.; Johnston, C.E.A.
〖参考〗Saunders, D.; Lawrie, K.W.M.; Crowe, A.M.; Johnston, C.E.A.; The synthesis of [14C]pantoprazole - SK&F 96022Z - An H+/K+ ATP inhibitor. J Label Compd Radiopharm , 409
〖出处〗J Label Compd Radiopharm):409
〖备注〗A new synthesis of [14C]-labeled pantoprazole has been described:
1) The cyclization of potassium [14C]-ethylxanthate (I) with the diaminobenzene (II) by means of NaOH gives the imidazole (III), which is condensed with 2-(chloromethyl)-3,4-dimethoxypyridine (IV) by means of NaOH in ethanol to afford the sulfide (V). Finally this compound is oxidized with m-chloroperbenzoic acid (mcpba) in dichloromethane (Scheme a).
2) Using [14C]-labeled (IV)in the preceding synthesis, pantoprazole labeled in the methylene was obtained. Intermediate (IV) labeled in the methylene attached to the pyridine ring can be prepared as follows:
The reaction of 2-bromo-3,4-dimethoxypyridine (V) with [14C]-labeled CuCN gives 3,4-dimethoxypyridine-2-carbonitrile (VI), which is hydrolyzed with NaOH and methylated with diazomethane to the methyl ester (VII). Finally this compound is reduced with LiAlH4 to the corresponding alcohol and treated with SOCl2 to give the chloromethylpyridine (IV*) with the [14C] label. Then this compound is condensed with benzimidazole (III) as usual.(Scheme a).
〖来源〗J Med Chem
〖合成路线〗
〖标题〗(H+,K+)-ATPase inhibiting 2-[(2-pyridylmethyl)sulfinyl]benzimidazoles. 4. A novel series of dimethoxypyridyl-substituted inhibitors with enhanced selectivity. The selection of pantoprazole as a clinical candidate
〖合成方法〗3-Methoxy-2-methylpyridine (VII), prepared by methylation of 2-methyl-3-pyridinol (VI), was converted to the N-oxide (VIII) employing peracetic acid. Nitration of the pyridine N-oxide (VIII) with concentrated nitric acid gave the 4-nitro derivative (IX). Subsequent displacement of the nitro group of (IX) by sodium methoxide led to the dimethoxypyridine N-oxide (X). Rearrangement of the N-oxide group of (X) in hot acetic anhydride produced the acetoxymethyl pyridine (XI). After basic hydrolysis of the acetate ester (XI), the resultant hydroxymethyl pyridine (XII) was chlorinated by SOCl2, yielding chloride (XIII). Condensation between mercapto benzimidazole (V) and the chloromethyl pyridine (XIII) in ethanolic NaOH led to the sulfide adduct (XIV). This was finally oxidized to the desired sulfoxide by using meta-chloroperbenzoic acid in CH2Cl2. The oxidation of sulfide (XIV) has also been performed employing sodium perborate, sodium percarbonate in the presence of ammonium molybdate, or tert-butyl hydroperoxide in the presence of vanadyl acetylacetonate.
〖作者〗Kohl, B.; Sturm, E.; Senn-Bilfinger, J.; Simon, W.A.; Krger, U.; Schaefer, H.; Rainer, G.; Figala, V.; Klemm, K.
〖参考〗Kohl, B.; Sturm, E.; Senn-Bilfinger, J.; Simon, W.A.; Krger, U.; Schaefer, H.; Rainer, G.; Figala, V.; Klemm, K.; (H+,K+)-ATPase inhibiting 2-[(2-pyridylmethyl)sulfinyl]benzimidazoles. 4. A novel series of dimethoxypyridyl-substituted inhibitors with enha (free base)/li>
li>??p耀?Losartan potassium, L-158086, MK-0954, E-3340, MK-954, Ex-89(f
〖出处〗J Med Chem):1049
〖备注〗The synthesis of IY-81149 can be obtained according to Scheme a. The oxidation of 2,3-lutidine (I) with hydrogen peroxide in acetic acid affords 2,3-dimethylpyridine-N-oxide (II), which is treated with sulfuric acid and nitric acid to give the corresponding nitro compound (III). The treatment of (III) with NaOH in methanol gives 2,3-dimethyl-4-methoxypyridine-N-oxide (IV), which is reacted with acetic acid and acetic anhydride and oxidated in refluxing NaOH, yielding 3-methyl-4-methoxypyridine-2-methanol (V). The chlorination of (V) with thionylchloride in CH2Cl2 affords 3-methyl-4-methoxy-2-chloromethylpyridine (VI). The reaction of 2-mercapto-5-nitrobenzimidazole (VII) with iron and concentrated HCl in refluxing ethanol and water gives monoamine (VIII), which by condensation with 2,5-dimethoxytetrahydrofuran (IX) in acetic acid yields 2-mercapto-5-(1-pyrrolyl)benzimidazole (X). The condensation of (VI) with (X) by means of NaOH in methanol gives 2-[(4-methoxy-3-methyl-2-pyridinyl)methylsulfanyl]-5-(1H-pyrrol-1-yl)-1H-benzimidazole (XI), which is finally treated with m-chloroperoxybenzoic acid (m-CPBA) in chloroform.
Description
Pale yellow crystalline powder, m.p. 152-5 C.
〖来源〗EP 0134400; JP ; JP ; US 4555518
〖合成路线〗
〖标题〗Antisecretory substd. pyridylmethylthio-(or sulfinyl)benzimidazoles
〖合成方法〗The precursor 5-(difluoromethoxy)-2-mercaptobenzimidazole (V) was prepared by the following route. Nitration of N-(p-difluoromethoxyphenyl)acetamide (I) provided nitro anilide (II), which was hydrolyzed to the corresponding nitro aniline (III) employing methanolic NaOMe. Reduction of (III) to the phenylenediamine (IV) was performed by catalytic hydrogenation over Pd/C. Then, cyclization of diamine (IV) with potassium O-ethyl dithiocarbonate gave rise to the benzimidazole (V).
〖作者〗Rainer, G.; Riedel, R.; Senn-Bilfinger, J.; Klemm, K.; Schaefer, H.; Figala, V. (Altana Pharma Deutschland GmbH )
〖参考〗Rainer, G.; Riedel, R.; Senn-Bilfinger, J.; Klemm, K.; Schaefer, H.; Figala, V. (Altana Pharma Deutschland GmbH ); Antisecretory substd. pyridylmethylthio-(or sulfinyl)benzimidazoles. EP 0134400; JP ; JP ; US 4555518
〖出处〗EP 0134400; JP ; JP ; US 4555518,,():
〖来源〗AU 8543640; EP 0166287; JP ; US 4758579
〖合成路线〗
〖标题〗Dialkoxypyridines, process for their preparation, their use and medicines containing them
〖合成方法〗The precursor 5-(difluoromethoxy)-2-mercaptobenzimidazole (V) was prepared by the following route. Nitration of N-(p-difluoromethoxyphenyl)acetamide (I) provided nitro anilide (II), which was hydrolyzed to the corresponding nitro aniline (III) employing methanolic NaOMe. Reduction of (III) to the phenylenediamine (IV) was performed by catalytic hydrogenation over Pd/C. Then, cyclization of diamine (IV) with potassium O-ethyl dithiocarbonate gave rise to the benzimidazole (V).
〖作者〗Kohl, B.; Sturm, E.; Klemm, K.; Riedel, R.; Figala, V.; Rainer, G.; Schaefer, H.; Senn-Bilfinger, J. (Altana Pharma Deutschland GmbH )
〖参考〗Kohl, B.; Sturm, E.; Klemm, K.; Riedel, R.; Figala, V.; Rainer, G.; Schaefer, H.; Senn-Bilfinger, J. (Altana Pharma Deutschland GmbH ); Dialkoxypyridines, process for their preparation, their use and medicines containing them. AU 8543640; EP 0166287; JP -7 (free base)
〖出处〗AU 8543640; EP 0166287; JP ; US 4758579,,():
〖来源〗WO 9947514
〖合成路线〗
〖标题〗Chemical process for the production of sulphinyl derivs. by oxidation of the corresponding co-derivs. with perborates
〖合成方法〗3-Methoxy-2-methylpyridine (VII), prepared by methylation of 2-methyl-3-pyridinol (VI), was converted to the N-oxide (VIII) employing peracetic acid. Nitration of the pyridine N-oxide (VIII) with concentrated nitric acid gave the 4-nitro derivative (IX). Subsequent displacement of the nitro group of (IX) by sodium methoxide led to the dimethoxypyridine N-oxide (X). Rearrangement of the N-oxide group of (X) in hot acetic anhydride produced the acetoxymethyl pyridine (XI). After basic hydrolysis of the acetate ester (XI), the resultant hydroxymethyl pyridine (XII) was chlorinated by SOCl2, yielding chloride (XIII). Condensation between mercapto benzimidazole (V) and the chloromethyl pyridine (XIII) in ethanolic NaOH led to the sulfide adduct (XIV). This was finally oxidized to the desired sulfoxide by using meta-chloroperbenzoic acid in CH2Cl2. The oxidation of sulfide (XIV) has also been performed employing sodium perborate, sodium percarbonate in the presence of ammonium molybdate, or tert-butyl hydroperoxide in the presence of vanadyl acetylacetonate.
〖作者〗Brennan, J.P.; Turner, A.T. (Abbott Laboratories Inc.)
〖参考〗Brennan, J.P.; Turner, A.T. (Abbott Laboratories Inc.); Chemical process for the production of sulphinyl derivs. by oxidation of the corresponding co-derivs. with perborates. WO 9947514
〖出处〗WO 9947514,,():
〖来源〗ES 2163372; WO 0168594
〖合成路线〗
〖标题〗Method for oxidizing a thioether group into a sulfoxide group
〖合成方法〗3-Methoxy-2-methylpyridine (VII), prepared by methylation of 2-methyl-3-pyridinol (VI), was converted to the N-oxide (VIII) employing peracetic acid. Nitration of the pyridine N-oxide (VIII) with concentrated nitric acid gave the 4-nitro derivative (IX). Subsequent displacement of the nitro group of (IX) by sodium methoxide led to the dimethoxypyridine N-oxide (X). Rearrangement of the N-oxide group of (X) in hot acetic anhydride produced the acetoxymethyl pyridine (XI). After basic hydrolysis of the acetate ester (XI), the resultant hydroxymethyl pyridine (XII) was chlorinated by SOCl2, yielding chloride (XIII). Condensation between mercapto benzimidazole (V) and the chloromethyl pyridine (XIII) in ethanolic NaOH led to the sulfide adduct (XIV). This was finally oxidized to the desired sulfoxide by using meta-chloroperbenzoic acid in CH2Cl2. The oxidation of sulfide (XIV) has also been performed employing sodium perborate, sodium percarbonate in the presence of ammonium molybdate, or tert-butyl hydroperoxide in the presence of vanadyl acetylacetonate.
〖作者〗Coppi, L.; Campon Pardo, J.; Berenguer Maimo, R. (Laboratorios del Dr. Esteve, SA)
〖参考〗Coppi, L.; Campon Pardo, J.; Berenguer Maimo, R. (Laboratorios del Dr. Esteve, SA); Method for oxidizing a thioether group into a sulfoxide group. ES 2163372; WO 0168594
〖出处〗ES 2163372; WO 0168594,,():
〖来源〗ES 2171116; WO 0179194
〖合成路线〗
〖标题〗Method for obtaining derivs. of [[pyridyl substd.)methyl]thio]benzimidazol
〖合成方法〗3-Methoxy-2-methylpyridine (VII), prepared by methylation of 2-methyl-3-pyridinol (VI), was converted to the N-oxide (VIII) employing peracetic acid. Nitration of the pyridine N-oxide (VIII) with concentrated nitric acid gave the 4-nitro derivative (IX). Subsequent displacement of the nitro group of (IX) by sodium methoxide led to the dimethoxypyridine N-oxide (X). Rearrangement of the N-oxide group of (X) in hot acetic anhydride produced the acetoxymethyl pyridine (XI). After basic hydrolysis of the acetate ester (XI), the resultant hydroxymethyl pyridine (XII) was chlorinated by SOCl2, yielding chloride (XIII). Condensation between mercapto benzimidazole (V) and the chloromethyl pyridine (XIII) in ethanolic NaOH led to the sulfide adduct (XIV). This was finally oxidized to the desired sulfoxide by using meta-chloroperbenzoic acid in CH2Cl2. The oxidation of sulfide (XIV) has also been performed employing sodium perborate, sodium percarbonate in the presence of ammonium molybdate, or tert-butyl hydroperoxide in the presence of vanadyl acetylacetonate.
〖作者〗Coppi, L.; Berenguer Maim? R. (Laboratorios del Dr. Esteve, SA)
〖参考〗Coppi, L.; Berenguer Maim? R. (Laboratorios del Dr. Esteve, SA); Method for obtaining derivs. of [[pyridyl substd.)methyl]thio]benzimidazol. ES 2171116; WO 0179194
〖出处〗ES 2171116; WO 0179194,,():
〖来源〗WO 0262786
〖合成路线〗
〖标题〗Processes for the production of substd. 2-(2-pyridylmethyl) sulfinyl-1H-benzimidazoles
〖合成方法〗3-Methoxy-2-methylpyridine (VII), prepared by methylation of 2-methyl-3-pyridinol (VI), was converted to the N-oxide (VIII) employing peracetic acid. Nitration of the pyridine N-oxide (VIII) with concentrated nitric acid gave the 4-nitro derivative (IX). Subsequent displacement of the nitro group of (IX) by sodium methoxide led to the dimethoxypyridine N-oxide (X). Rearrangement of the N-oxide group of (X) in hot acetic anhydride produced the acetoxymethyl pyridine (XI). After basic hydrolysis of the acetate ester (XI), the resultant hydroxymethyl pyridine (XII) was chlorinated by SOCl2, yielding chloride (XIII). Condensation between mercapto benzimidazole (V) and the chloromethyl pyridine (XIII) in ethanolic NaOH led to the sulfide adduct (XIV). This was finally oxidized to the desired sulfoxide by using meta-chloroperbenzoic acid in CH2Cl2. The oxidation of sulfide (XIV) has also been performed employing sodium perborate, sodium percarbonate in the presence of ammonium molybdate, or tert-butyl hydroperoxide in the presence of vanadyl acetylacetonate.
〖作者〗Mendelovici, M.; Avrutov, I. (Teva Pharmaceutical Industries Ltd.; Teva Pharmaceuticals USA, Inc.)
〖参考〗Mendelovici, M.; Avrutov, I. (Teva Pharmaceutical Industries Ltd.; Teva Pharmaceuticals USA, Inc.); Processes for the production of substd. 2-(2-pyridylmethyl) sulfinyl-1H-benzimidazoles. WO 0262786
〖出处〗WO 0262786,,():
〖来源〗WO 9850361
〖合成路线〗
〖标题〗Synthesis of pharmaceutically useful pyridine derivs.
〖合成方法〗A related method for the preparation of the intermediate 3,4-dimethoxy-2-(hydroxymethyl)pyridine (XII) has been disclosed. 3-Methoxypyridine (XV) was chlorinated to (XVI) by refluxing in SOCl2. Radical carboxylation of pyridine (XVI) was carried out by reaction with ethyl pyruvate in the presence of hydrogen peroxide and iron(II) sulfate. The resultant ethyl 4-chloro-3-methoxypicolinate (XVII) was then converted to the dimethoxypicolinate (XVIII) by treatment with sodium methoxide. Then, ester group reduction in (XVIII) by means of DIBAL provided the target hydroxymethyl pyridine (XII).
〖作者〗Chen, L.; Zoghbi, M. (PDi-Research Laboratories, Inc. )
〖参考〗Chen, L.; Zoghbi, M. (PDi-Research Laboratories, Inc. ); Synthesis of pharmaceutically useful pyridine derivs.. WO 9850361
〖出处〗WO 9850361,,():
〖来源〗ES 2171116; WO 0179194
〖合成路线〗
〖标题〗Method for obtaining derivs. of [[pyridyl substd.)methyl]thio]benzimidazol
〖合成方法〗In an alternative procedure, the nitropyridine N-oxide (IX) was rearranged to the (mesyloxymethyl)pyridine (XIX) by treatment with methanesulfonic anhydride. Condensation of mesylate (XIX) with mercaptobenzimidazole (V), with concomitant nitro group displacement in the presence of sodium methoxide led to the sulfide precursor (XIV). This was then oxidized to the title sulfoxide employing sodium percarbonate and ammonium molybdate. An analogous synthetic route starting from the chloropyridine N-oxide (XX) provided mesylate (XXI), which was condensed with (V) in the presence of Et3N, leading to the sulfide adduct (XXII). The 4-chloro group of (XXII) was then displaced by sodium methoxide producing the dimethoxypyridine derivative (XIV).
〖作者〗Coppi, L.; Berenguer Maim? R. (Laboratorios del Dr. Esteve, SA)
〖参考〗Coppi, L.; Berenguer Maim? R. (Laboratorios del Dr. Esteve, SA); Method for obtaining derivs. of [[pyridyl substd.)methyl]thio]benzimidazol. ES 2171116; WO 0179194
〖出处〗ES 2171116; WO 0179194,,():
〖来源〗WO 0228852
〖合成路线〗
〖标题〗A process for the preparation of pantoprazole and intermediates therefor
〖合成方法〗Similarly, rearrangement of the chloropyridine N-oxide (XX) using acetic anhydride produced acetate ester (XXIII), which was further hydrolyzed to the pyridine alcohol (XXIV). The chloromethyl pyridine (XXV), obtained by treatment of alcohol (XXIV) with SOCl2, was condensed with the mercaptobenzimidazole (V) in the presence of tetramethylguanidine producing sulfide (XXII). Conversion of (XXII) to the title compound was then performed by oxidation to sulfoxide (XXVI) employing sodium percarbonate, followed by chloride displacement with potassium methoxide.
〖作者〗Palomo Coll, A.
〖参考〗Palomo Coll, A.; A process for the preparation of pantoprazole and intermediates therefor. WO 0228852
〖出处〗WO 0228852,,():
本文导航：
Pantoprazole sodium, DZ-2352a, B-8510-29(free acid), By-1023
上一篇：暂无}