公开(公告)号：US20100056785A1

公开(公告)日：2010-03-04

申请号：US12595663

申请日：2008-04-10

Applicant: Om Dutt Tyagi ,  Tushar Kumar Srivastava ,  Vellanki Siva Ram Prasad ,  Dnyandev Ragho Rane ,  Bandi Naga Durga Rao ,  Daggula Srinivas Reddy

Inventor： Om Dutt Tyagi ,  Tushar Kumar Srivastava ,  Vellanki Siva Ram Prasad ,  Dnyandev Ragho Rane ,  Bandi Naga Durga Rao ,  Daggula Srinivas Reddy

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: Present invention relates to an improved process for the preparation of Zopiclone and its enantiomerically enriched isomer (Eszopiclone). 6-(5-Chloropyridin-2-yl)-5-hydroxy-7-oxo-5,6-dihydropyrrolo[3,4-b]pyrazine is reacted with 1-chloro-carbonyl-4-methylpiperazine in the presence of alkali earth metal carbonates, hydroxides or oxides in a solvent medium to give Zopiclone. It is reacted with optically active acid in a mixture of water and water miscible organic solvent followed by work up to give Eszopiclone. The present invention also relates to process for the conversion of (R) or (S) Zopiclone to 6-(5-chloropyrid-2-yl)-5-hydroxy-7-oxo-5,6-dihydro-pyrrolo-[3,4-b]-pyrazine of the intermediate which can be converted to racemic Zopiclone.

Abstract translation: 本发明涉及一种改良的佐匹克隆及其对映体富集异构体（依佐替普）的制备方法。 6-（5-氯吡啶-2-基）-5-羟基-7-氧代-5,6-二氢吡咯并[3,4-b]吡嗪在碱存在下与1-氯 - 羰基-4-甲基哌嗪反应 土壤金属碳酸盐，氢氧化物或氧化物在溶剂介质中给予佐匹克隆。 将其与光学活性酸在水和水混溶性有机溶剂的混合物中反应，随后加工得到依佐替普。 本发明还涉及将（R）或（S）佐匹克隆转化为6-（5-氯吡啶-2-基）-5-羟基-7-氧代-5,6-二氢 - 吡咯并[3 ，4-b] - 吡嗪，其可以转化为外消旋佐匹克隆。

公开(公告)号：US07427692B2

公开(公告)日：2008-09-23

申请号：US11360283

申请日：2006-02-23

Applicant: Om Dutt Tyagi ,  Dnyandev Ragho Rane ,  Tushar Kumar Srivastava ,  Krishnarao Tukaram Sirsath

Inventor： Om Dutt Tyagi ,  Dnyandev Ragho Rane ,  Tushar Kumar Srivastava ,  Krishnarao Tukaram Sirsath

IPC: C07C51/56

CPC classification number: C07D501/00 ,  C07C229/34 ,  C07F7/1804

Abstract: A process for preparation of 7-[D-α-amino-α-(4-hydroxyphenyl)acetamido]-3-(1-propen-1-yl)-3-cephem-4-carboxylic acid viz. Cefprozil of formula (I) in high purity, substantially free of impurities, which comprises preparation of mixed acid anhydride by selecting the sequence and temperature of addition of the reagents and its subsequent condensation with a protected 7-APCA; followed by hydrolysis, isolation and purification to give Cefprozil of formula (I) in the form of a monohydrate.

Abstract translation: 制备7- [D-α-氨基-α-（4-羟基苯基）乙酰氨基] -3-（1-丙烯-1-基）-3-头孢烯-4-羧酸的方法， 式（I）的头孢司列高纯度，基本上不含杂质，其包括通过选择加入试剂的顺序和温度及随后与受保护的7-APCA缩合制备混合酸酐; 然后水解，分离和纯化，得到一水合物形式的式（I）的头孢普利。

公开(公告)号：US07728136B2

公开(公告)日：2010-06-01

申请号：US11630054

申请日：2005-06-16

Applicant: Om Dutt Tyagi ,  Tushar Kumar Srivastava ,  Yogendra Kumar Chauhan ,  Vasanth Kumar Nalam

Inventor： Om Dutt Tyagi ,  Tushar Kumar Srivastava ,  Yogendra Kumar Chauhan ,  Vasanth Kumar Nalam

IPC: C07D419/06

CPC classification number: C07D417/12

Abstract: A novel method for preparing a compound of formula I which comprises of coupling the piperazine derivative of formula II with alkyl halide containing compound of the formula III by heating in solvent free conditions or, optionally, in a minimum quantity of non-aqueous suspending liquid, in presence of a catalyst and a neutralizing agent to neutralize the hydrohalic acid.

Abstract translation: 一种制备式I化合物的新方法，其包括将式II的哌嗪衍生物与含有式III的化合物的烷基卤化合物在无溶剂条件下加热，或任选地在最少量的非水性悬浮液中偶联， 在催化剂和中和剂存在下中和氢卤酸。

公开(公告)号：US07230097B2

公开(公告)日：2007-06-12

申请号：US10801443

申请日：2004-03-15

Applicant: Om Dutt Tyagi ,  Dnyandev Ragho Rane ,  Tushar Kumar Srivastava ,  Krishnarao Tukaram Sirsath

Inventor： Om Dutt Tyagi ,  Dnyandev Ragho Rane ,  Tushar Kumar Srivastava ,  Krishnarao Tukaram Sirsath

IPC: C07D501/22 ,  C07D501/04

CPC classification number: C07D501/00 ,  C07C229/34 ,  C07F7/1804

Abstract: A process for preparation of 7-[D-α-amino-α-(4-hydroxyphenyl)acetamido]-3-(1-propen-1-yl)-3-cephem-4-carboxylic acid viz. Cefprozil of formula (I) in high purity, substantially free of impurities, which comprises preparation of mixed acid anhydride by selecting the sequence and temperature of addition of the reagents and its subsequent condensation with a protected 7-APCA; followed by hydrolysis, isolation and purification to give Cefprozil of formula (I) in the form of a monohydrate.

Abstract translation: 制备7- [D-α-氨基-α-（4-羟基苯基）乙酰氨基] -3-（1-丙烯-1-基）-3-头孢烯-4-羧酸的方法， 式（I）的头孢司列高纯度，基本上不含杂质，其包括通过选择加入试剂的顺序和温度及随后与受保护的7-APCA缩合制备混合酸酐; 然后进行水解，分离和纯化，得到一水合物形式的式（I）的头孢普利。

公开(公告)号：US08309723B2

公开(公告)日：2012-11-13

申请号：US12595663

申请日：2008-04-10

Applicant: Om Dutt Tyagi ,  Tushar Kumar Srivastava ,  Vellanki Siva Ram Prasad ,  Dnyandev Ragho Rane ,  Bandi Naga Durga Rao ,  Daggula Srinivas Reddy

Inventor： Om Dutt Tyagi ,  Tushar Kumar Srivastava ,  Vellanki Siva Ram Prasad ,  Dnyandev Ragho Rane ,  Bandi Naga Durga Rao ,  Daggula Srinivas Reddy

IPC: C07D495/00

CPC classification number: C07D487/04

Abstract: Present invention relates to an improved process for the preparation of Zopiclone and its enantiomerically enriched isomer (Eszopiclone). 6-(5-Chloropyridin-2-yl)-5-hydroxy-7-oxo-5,6-dihydropyrrolo[3,4-b]pyrazine is reacted with 1-chloro-carbonyl-4-methylpiperazine in the presence of alkali earth metal carbonates, hydroxides or oxides in a solvent medium to give Zopiclone. It is reacted with optically active acid in a mixture of water and water miscible organic solvent followed by work up to give Eszopiclone. The present invention also relates to process for the conversion of (R) or (S) Zopiclone to 6-(5-chloropyrid-2-yl)-5-hydroxy-7-oxo-5,6-dihydro-pyrrolo-[3,4-b]-pyrazine of the intermediate which can be converted to racemic Zopiclone.

Abstract translation: 本发明涉及一种改良的佐匹克隆及其对映体富集异构体（依佐替普）的制备方法。 6-（5-氯吡啶-2-基）-5-羟基-7-氧代-5,6-二氢吡咯并[3,4-b]吡嗪在碱存在下与1-氯 - 羰基-4-甲基哌嗪反应 土壤金属碳酸盐，氢氧化物或氧化物在溶剂介质中给予佐匹克隆。 将其与光学活性酸在水和水混溶性有机溶剂的混合物中反应，随后加工得到依佐替普。 本发明还涉及将（R）或（S）佐匹克隆转化为6-（5-氯吡啶-2-基）-5-羟基-7-氧代-5,6-二氢 - 吡咯并[3 ，4-b] - 吡嗪，其可以转化为外消旋佐匹克隆。