公开(公告)号：US07196216B2

公开(公告)日：2007-03-27

申请号：US10497899

申请日：2002-11-18

Applicant: Jagdish Chand Saigal ,  Rajender Pershad Gupta ,  Rajesh Vinodrai Naik ,  Araddy Rajshekhar ,  Rajesh Dilip Joshi

Inventor： Jagdish Chand Saigal ,  Rajender Pershad Gupta ,  Rajesh Vinodrai Naik ,  Araddy Rajshekhar ,  Rajesh Dilip Joshi

IPC: C07C61/08

CPC classification number: C07C227/42 ,  C07C229/28

Abstract: A process for producing gabapentin, (1-(aminomethyl)-1-cyclohexaneacetic acid) from gabapentin hydrochloride salt. In the disclosed process, the gabapentin hydrochloride is converted to gabapentin using an inorganic base, such as barium hydroxide. Gabapentin hydrochloride is converted to gabapentin sulfate which in turn is converted to free base using barium hydroxide. The process is directed to improvement in the manufacture of gabapentin which would be industrially feasible and effective. Gabapentin obtained following the process of the invention is suitable as a drug especially in the treatment of cerebral diseases such as epilepsy.

Abstract translation: 加巴喷丁盐酸盐生产加巴喷丁（1-（氨基甲基）-1-环己烷乙酸）的方法。 在所公开的方法中，使用无机碱如氢氧化钡将加巴喷丁盐酸盐转化为加巴喷丁。 将加巴喷丁盐酸盐转化为硫酸加巴喷丁，其又使用氢氧化钡转化为游离碱。 该方法旨在改善在工业上可行和有效的加巴喷丁的制造。 按照本发明的方法获得的加巴喷丁适合作为特别是治疗脑疾病如癫痫的药物。

公开(公告)号：US20120116093A1

公开(公告)日：2012-05-10

申请号：US13263397

申请日：2009-11-19

Applicant: Prakash Yashwant Kolhe ,  Rajesh Dilip Joshi ,  Bimal Kumar Srivastava ,  Nitin Jerambhai Patel ,  Sanket Sureshbhai Gajjar

Inventor： Prakash Yashwant Kolhe ,  Rajesh Dilip Joshi ,  Bimal Kumar Srivastava ,  Nitin Jerambhai Patel ,  Sanket Sureshbhai Gajjar

IPC: C07D403/10

CPC classification number: C07D403/10

Abstract: A one pot process for the synthesis of Irbesartan comprising reacting 2-n-Butyl-1,3-Diazaspiro[4,4]Non-1-en-4-one (Formula III) and Bromomethyl Cyanobiphenyl (Formula IV) in the presence of base and water with the optional use of PTC to give formula II from which Irbesartan is obtained by reacting with sodium azide and triethylamine hydrochloride in the presence of a non polar solvent.

Abstract translation: 一种用于合成厄贝沙坦的一种方法，其包括在存在下使2-正丁基-1,3-二氮杂螺[4,4]壬-1-烯-4-酮（式III）和溴甲基氰基联苯（式IV） 的碱和水，可选地使用PTC得到式II，其中通过与非极性溶剂的存在下，与叠氮化钠和三乙胺盐酸盐反应从其获得厄贝沙坦。

公开(公告)号：US08609859B2

公开(公告)日：2013-12-17

申请号：US13263397

申请日：2009-11-19

Applicant: Prakash Yashwant Kolhe ,  Rajesh Dilip Joshi ,  Bimal Kumar Srivastava ,  Nitin Jerambhai Patel ,  Sanket Sureshbhai Gajjar

Inventor： Prakash Yashwant Kolhe ,  Rajesh Dilip Joshi ,  Bimal Kumar Srivastava ,  Nitin Jerambhai Patel ,  Sanket Sureshbhai Gajjar

IPC: C07D403/10 ,  C07D233/32

CPC classification number: C07D403/10

Abstract: A one pot process for the synthesis of Irbesartan comprising reacting 2-n-Butyl-1,3-Diazaspiro[4,4]Non-1-en-4-one (Formula III) and Bromomethyl Cyanobiphenyl (Formula IV) in the presence of base and water with the optional use of PTC to give formula II from which Irbesartan is obtained by reacting with sodium azide and triethylamine hydrochloride in the presence of a non polar solvent.

Abstract translation: 一种用于合成厄贝沙坦的一种方法，其包括在存在下使2-正丁基-1,3-二氮杂螺[4,4]壬-1-烯-4-酮（式III）和溴甲基氰基联苯（式IV） 的碱和水，可选地使用PTC得到式II，其中通过与非极性溶剂的存在下，与叠氮化钠和三乙胺盐酸盐反应从其获得厄贝沙坦。