公开(公告)号：EP0906278B1

公开(公告)日：2002-10-16

申请号：EP97928831.3

申请日：1997-05-28

申请人： SCHERING CORPORATION

发明人： WU, Guang-Zhong ,  CHEN, Xing ,  WONG, Yee-Shing ,  SCHUMACHER, Doris, P. ,  STEINMAN, Martin

IPC分类号： C07D205/08

CPC分类号： C07D205/08

摘要： The invention relates to a process for producing a compound of formula (I) wherein R1, R2 and R3 are as defined in the specification, which comprises reacting a lactone with an imine to obtain a chiral diol of formula (IV) oxidizing the diol, condensing the resultant aldehyde with an enolether, hydrogenating the product, and chirally catalytically reducing the resultant ketone.

公开(公告)号：EP0991640A1

公开(公告)日：2000-04-12

申请号：EP98928873.3

申请日：1998-06-15

申请人： SCHERING CORPORATION

发明人： CHEN, Xing ,  POIRIER, Marc ,  WONG, Yee-Shing ,  WU, Guang-Zhong

IPC分类号： C07D401/12

CPC分类号： C07D401/04

摘要： The invention relates to a process for preparing a compound of formula (I), comprising: (a) reacting 2,5-dibromo-3-methylpyridine with an amine of the formula NHR5R6 to obtain an amide; (b) reacting the amide with a compound of formula (3) in the presence of a strong base to obtain a compound of formula (4); (c) converting a compound of formula (4) to the corresponding cyano compound or aldehyde; (d) reacting the cyano compound or aldehyde with a piperidine derivative to obtain an aldehyde or alcohol of formula (7a) or (7b), respectively; (e) cyclizing a compound of formula (7a) or (7b); wherein R1-R7 are as defined in the specification.

公开(公告)号：EP0906278A1

公开(公告)日：1999-04-07

申请号：EP97928831.0

申请日：1997-05-28

申请人： SCHERING CORPORATION

发明人： WU, Guang-Zhong ,  CHEN, Xing ,  WONG, Yee-Shing ,  SCHUMACHER, Doris, P. ,  STEINMAN, Martin

IPC分类号： C07D205

CPC分类号： C07D205/08

摘要： The invention relates to a process for producing a compound of formula (I) wherein R1, R2 and R3 are as defined in the specification, which comprises reacting a lactone with an imine to obtain a chiral diol of formula (IV) oxidizing the diol, condensing the resultant aldehyde with an enolether, hydrogenating the product, and chirally catalytically reducing the resultant ketone.

公开(公告)号：EP0977739A1

公开(公告)日：2000-02-09

申请号：EP98910084.7

申请日：1998-03-23

申请人： SCHERING CORPORATION

发明人： CHEN, Xing ,  POIRIER, Marc ,  WONG, Yee-Shing ,  WU, Guang-Zhong

IPC分类号： C07D221/16 ,  C07D213/81 ,  C07C25/02 ,  C07C17/16

CPC分类号： C07D213/81 ,  C07C17/16 ,  C07C25/02 ,  C07D221/16

摘要： The invention relates to a process for preparing a compound of formula (I), comprising reacting a bromo-substituted pyridine with an amine of the formula NHR5R6, reacting the resulting amide with an iodo-halomethyl-substituted compound and cyclizing the resultant product, wherein R, R?1, R2, R3 and R4¿ are as defined in the specification; also claimed are a compound of formula (a), and a process for preparing it from the corresponding halo-substituted benzoic acid.

公开(公告)号：EP0977739B1

公开(公告)日：2003-10-29

申请号：EP98910084.7

申请日：1998-03-23

申请人： SCHERING CORPORATION

发明人： CHEN, Xing ,  POIRIER, Marc ,  WONG, Yee-Shing ,  WU, Guang-Zhong

IPC分类号： C07D221/16 ,  C07D213/81 ,  C07C25/02 ,  C07C17/16

CPC分类号： C07D213/81 ,  C07C17/16 ,  C07C25/02 ,  C07D221/16

摘要： The invention relates to a process for preparing a compound of formula (I), comprising reacting a bromo-substituted pyridine with an amine of the formula NHR5R6, reacting the resulting amide with an iodo-halomethyl-substituted compound and cyclizing the resultant product, wherein R, R?1, R2, R3 and R4¿ are as defined in the specification; also claimed are a compound of formula (a), and a process for preparing it from the corresponding halo-substituted benzoic acid.

公开(公告)号：EP0991640B1

公开(公告)日：2002-03-06

申请号：EP98928873.3

申请日：1998-06-15

申请人： SCHERING CORPORATION

发明人： CHEN, Xing ,  POIRIER, Marc ,  WONG, Yee-Shing ,  WU, Guang-Zhong

IPC分类号： C07D401/12

CPC分类号： C07D401/04

摘要： The invention relates to a process for preparing a compound of formula (I), comprising: (a) reacting 2,5-dibromo-3-methylpyridine with an amine of the formula NHR5R6 to obtain an amide; (b) reacting the amide with a compound of formula (3) in the presence of a strong base to obtain a compound of formula (4); (c) converting a compound of formula (4) to the corresponding cyano compound or aldehyde; (d) reacting the cyano compound or aldehyde with a piperidine derivative to obtain an aldehyde or alcohol of formula (7a) or (7b), respectively; (e) cyclizing a compound of formula (7a) or (7b); wherein R1-R7 are as defined in the specification.