公开(公告)号：WO0222849A3

公开(公告)日：2002-08-29

申请号：PCT/US0128409

申请日：2001-09-12

Applicant: SQUIBB BRISTOL MYERS CO ,  ZHU JINGYANG ,  YOU LI ,  WHITE BRENDA J ,  ZHAO SHANNON X ,  SKONEZNY PAUL M

Inventor： ZHU JINGYANG ,  YOU LI ,  WHITE BRENDA J ,  ZHAO SHANNON X ,  SKONEZNY PAUL M

IPC: C07B55/00 ,  C07C67/343 ,  C07C327/08 ,  C12P7/40 ,  C12P7/62 ,  C12P11/00 ,  C12P41/00 ,  C12R1/785 ,  C07B37/02

CPC classification number: H01M4/136 ,  C07C67/343 ,  C12P7/40 ,  C12P7/62 ,  C12P11/00 ,  C12P41/005 ,  H01M4/366 ,  H01M4/485 ,  H01M4/525 ,  H01M4/5825 ,  H01M4/625 ,  H01M10/052 ,  H01M10/0525 ,  H01M2004/027 ,  C07C69/738

Abstract: Provided is a method of resolving a racemic mixture of a compound of formula I to obtain a desired enantiomer, (I), wherein Ar is C6 or C10 aromatic group that can be substituted with H, C1 to C6 alkyl, trifluoromethyl or halo, R5 is halo or -S-R1, wherein R1 is H or acetyl, and R2 is H or C1 to C6 alkyl, the method comprising: reacting a compound of formula (I) wherein the compound is an ester whereby R2 is C1 to C6 alkyl with a lipase derived from Mucor meihei to stereoselectively hydrolyze the ester bond to produce an acid; and isolating the acid, wherein the reaction is conducted in a solvent comprising 80 % to 98% v/v % organic phase and a residue of water phase (which can be buffered).

Abstract translation: 提供了一种拆分式I化合物的外消旋混合物以获得所需的对映异构体（I）的方法，其中Ar是可被H，C 1至C 6烷基，三氟甲基或卤素取代的C 6或C 10芳族基团，R 5 是卤素或-S-R 1，其中R 1是H或乙酰基，R 2是H或C 1至C 6烷基，所述方法包括：使化合物是一种酯的式（I）化合物，其中R 2是C 1至C 6烷基 与来自美毛霉的脂肪酶立体选择性地水解酯键以产生酸; 并分离酸，其中反应在包含80％至98％v / v％有机相和水相残余物（可缓冲）的溶剂中进行。

公开(公告)号：WO2006074270A3

公开(公告)日：2006-07-13

申请号：PCT/US2006/000262

申请日：2006-01-05

Applicant: SCHERING CORPORATION ,  WU, Wenxue ,  D'SA, Bosco ,  LIANG, Feng ,  TRAN, Loc, Thanh ,  LEONG, William ,  DAHANUKAR, Vilas ,  ZAVIALOV, Ilia, A. ,  ORR, Cecilia ,  ZHAO, Shannon ,  LEE, Hong-chang ,  LIU, Yi ,  NGUYEN, Hoa, N. ,  SHIH, Xiongwei ,  ZHU, Man

Inventor： WU, Wenxue ,  D'SA, Bosco ,  LIANG, Feng ,  TRAN, Loc, Thanh ,  LEONG, William ,  DAHANUKAR, Vilas ,  ZAVIALOV, Ilia, A. ,  ORR, Cecilia ,  ZHAO, Shannon ,  LEE, Hong-chang ,  LIU, Yi ,  NGUYEN, Hoa, N. ,  SHIH, Xiongwei ,  ZHU, Man

IPC: C07D401/14 ,  C07D211/26

Abstract: The present invention is directed to the synthesis of 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine], and intermediates therefor from readily available starting materials by a novel route.

公开(公告)号：WO2006074270A2

公开(公告)日：2006-07-13

申请号：PCT/US2006000262

申请日：2006-01-05

Applicant: SCHERING CORP ,  WU WENXUE ,  D SA BOSCO ,  LIANG FENG ,  TRAN LOC THANH ,  LEONG WILLIAM ,  DAHANUKAR VILAS ,  ZAVIALOV ILIA A ,  ORR CECILIA ,  ZHAO SHANNON ,  LEE HONG-CHANG ,  LIU YI ,  NGUYEN HOA N ,  SHIH XIONGWEI ,  ZHU MAN

Inventor： WU WENXUE ,  D SA BOSCO ,  LIANG FENG ,  TRAN LOC THANH ,  LEONG WILLIAM ,  DAHANUKAR VILAS ,  ZAVIALOV ILIA A ,  ORR CECILIA ,  ZHAO SHANNON ,  LEE HONG-CHANG ,  LIU YI ,  NGUYEN HOA N ,  SHIH XIONGWEI ,  ZHU MAN

IPC: C07D401/14 ,  C07D211/26

CPC classification number: C07D211/96 ,  C07D211/26 ,  C07D401/14

Abstract: The present invention is directed to the synthesis of 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine], and intermediates therefor from readily available starting materials by a novel route.

Abstract translation: 本发明涉及4- [4 - [（R） - [1- [环丙基磺酰基] -4-哌啶基]（3-氟苯基）甲基] -3（S） - 甲基-1-哌嗪基] 1 - [（4,6-二甲基-5-嘧啶基）羰基] -4-甲基哌啶]，以及通过新途径从容易获得的起始原料中间产物。

公开(公告)号：WO2011024004A1

公开(公告)日：2011-03-03

申请号：PCT/GB2010/051417

申请日：2010-08-26

Applicant: ASTRAZENECA AB ,  ASTRAZENECA UK LIMITED ,  BIST, Shanta ,  EAKIN, Ann ,  SHERER, Brian ,  ZHAO, Shannon

Inventor： BIST, Shanta ,  EAKIN, Ann ,  SHERER, Brian ,  ZHAO, Shannon

IPC: C07D417/14 ,  A61P31/04 ,  A61K31/444 ,  C07F9/09

CPC classification number: C07D417/14 ,  C07F9/65583

Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.

Abstract translation: 描述式（I）化合物及其药学上可接受的盐。 还描述了其制备方法，含有它们的药物组合物，其作为药物的用途及其在治疗细菌感染中的用途。