CAS: 99294-93-6; Zolpidem Tartrate

📜2-氨基-5-甲基吡啶置于三溴化磷,碳酸氢钠,溶剂黄146体系中,用 四氢呋喃,甲醇,甲苯 作为反应溶剂,化学反应 3.75H,反应生成 酒石酸唑吡坦
参考文献:利用微波辅助化学三步快速组装唑吡坦及其氟化类似物的研究
标题:利用微波辅助化学三步快速组装唑吡坦及其氟化类似物的研究
摘要:我们开发了唑吡坦及其氟化类似物 1-3 的高效微波辅助三步合成.该程序依赖于易于获得且价格低廉的起始材料的利用.与传统加热系统相比,我们的协议在产品的产量和纯度方面表现出卓越的性能.值得注意的是,与油浴加热系统相比,完成反应所需的总时间要短得多.最后,我们对唑吡坦酒石酸盐 I 的制备进行了详细研究,并使用偏光显微镜评估了其粒径.我们的目标是选择合适的方法来产生可接受的粒度,因为固体大小直接影响生物流体中的溶解度和进一步的生物利用度.
DOI:10.3390/molecules25143161

专利信息

专利号:US-6921839-B2
优先权日:2000-08-29
标 题:Synthesis of N,N-dimethyl-3-(4-methyl) benzoyl propionamide a key intermediate of zolpidem
发明人：KUMAR YATENDRA; PRASAD MOHAN; NATH ASOK
权利人:RANBAXY LAB LTD
摘要:The present invention relates to an improved and industrially advantageous process for the preparation of N,N-dimethyl-3-(4-methyl)benzoyl propionamide of Formula I, n n nwhich is a key intermediate in the synthesis of zolpidem hemitartrate, a non-benzodiazepine hypnotic agent. The process includes reacting 3-(4-methyl)-benzoyl propionic acid of Formula IV, with alkyl chloroformate or pivaloyl chloride to get a mixed anhydride of Formula V; and reacting the mixed anhydride of Formula V with dimethylamine of Formula VI to get the N,N-dimethyl-3-(4-methyl)benzoyl propionamide of Formula I.

专利号:US-2005054669-A1
优先权日:2003-07-31
标 题 :Process for the synthesis of zolpidem
发明人：KUMAR YATENDRA; PRASAD MOHAN; NATH ASOK
摘要:The present invention relates to processes for the preparation of zolpidem of Formula V as shown in the accompanying drawings or pharmaceutically acceptable salts thereof from N,N-dimethyl-3-(4-methyl)benzoyl propionamide of Formula II. The process includes (a) reacting N,N-dimethyl-3-(4-methyl)benzoyl propionamide of Formula II with bromine to get the bromo amide of Formula III; (b) condensing the bromo amide of Formula III with 2-amino-5-methylpyridine of Formula IV to get the zolpidem base of Formula V; and (c) converting zolpidem base of Formula V to its hemitartarate salt of Formula VII.

专利号:EP-1370515-A2
优先权日:2000-08-29
标题:Synthesis of n,n-dimethyl-3-(4-methyl) benzoyl propionamide, a key intermediate of zolpidem

专利号:US-2004054230-A1
优先权日:2000-08-29
标 题 :Synthesis of n,n-dimethyl-3-(4-methyl) benzoyl propionamide a key intermediate of zolpidem

专利号:WO-2005010002-A1
优先权日:2003-07-31
标 题 :Process for the synthesis of zolpidem

专利号:WO-0218303-A3
优先权日:2000-08-29
标题:Synthesis of n,n-dimethyl-3-(4-methyl) benzoyl propionamide, a key intermediate of zolpidem