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：EP1556358B1

公开(公告)日：2007-06-20

申请号：EP03799375.5

申请日：2003-10-01

申请人： SCHERING CORPORATION

发明人： CHEN, Frank, X. ,  WONG, Yee-Shing ,  ECKERT, Jeffrey, M. ,  ZOU, Nanfei ,  LIANG, Feng ,  KIM-MEADE, Agnes, S. ,  POIRIER, Marc ,  THIRUVENGADAM, Tiruvettipuram, K. ,  WU, George, G.

IPC分类号： C07D221/00

CPC分类号： C07D401/14 ,  C07D221/16

摘要： An enantioselective process for preparing intermediates useful in the preparation of the chiral tricyclic compound of formula (I), is disclosed.

公开(公告)号：EP1131296A2

公开(公告)日：2001-09-12

申请号：EP99972525.2

申请日：1999-11-18

申请人： SCHERING CORPORATION

发明人： BERNARD, Charles, F. ,  CASEY, Michael ,  CHEN, Frank, Xing ,  GROGAN, Denise, C. ,  POIRIER, Marc ,  WILLIAMS, Robert, P. ,  WONG, Yee-Shing ,  WU, George, G.

IPC分类号： C07D221/16 ,  C07D213/81

CPC分类号： C07D221/16

摘要： A process for preparing a compound having formula (I) by (A) reacting a compound having formula (II), wherein R5 is aryl or heteroaryl, with a dehydrating agent to produce an imine having formula (IIa); and (B) hydrolyzing the imine produced in step (A) to produce the compound having formula (I). The imines and a process for preparing a compound having formula (III) are disclosed.

公开(公告)号：EP1274688B1

公开(公告)日：2006-12-20

申请号：EP01927122.0

申请日：2001-04-17

申请人： SCHERING CORPORATION

发明人： POIRIER, Marc ,  WONG, Yee-Shing ,  WU, George, G.

IPC分类号： C07D221/16 ,  C07D213/79

CPC分类号： C07D213/79 ,  C07D221/16

摘要： A process is provided for preparing a compound having the formula (I) comprising: (a) reacting a compound having the formula (II) with an isocyanate having the formula R1NCO to produce a compound having the formula (III); (b) optionally hydrolyzing the compound of formula (III) to form an amide having the formula (IV); (c) reacting the compound of formula (III) or the amide of formula (IV) with a compound having the formula (V) in the presence of a strong base to produce a compound having the formula (VI); and (d) cyclizing the compound of formula (VI) to obtain the compound of formula (I), wherein R is H or Cl; M is selected from the group consisting of Li, Na, K, MgX, ZnRA, and Al(RA)2; RA is alkyl; X is halo; R1 is selected from the group consisting of alkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, and heterocycloalkylalkyl; and L is a leaving group. Also provided is a process for preparing a compound having the formula (VIII) comprising reacting a compound having the formula (II) with CO¿2? and a protonating agent to obtain the compound of formula (VIII), wherein M is selected from the group consisting of Li, Na, K, MgX, ZnR?A¿, and Al(RA)2, wherein RA is alkyl and X is halo.

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：EP1966233A1

公开(公告)日：2008-09-10

申请号：EP06851460.3

申请日：2006-11-13

申请人： Schering Corporation

发明人： WU, George, G. ,  XIE, Ji ,  RASHATASAKHON, Paitoon ,  CHEN, Frank, Xing ,  POIRIER, Marc ,  SPRAGUE, Victoria, M.

IPC分类号： C07K5/02 ,  C07D209/52

CPC分类号： C07D209/52 ,  A61K38/00 ,  C07K5/0202

摘要： The present application relates to a process for preparing a compound of formula I: wherein R1 is alkyl; R2 is alkyl; and R3 is optionally substituted cycloalklylalkyl which comprises oxidizing a compound of the formula wherein R1, R2 and R3 are defined above to yield a compound of formula I.

公开(公告)号：EP1274688A1

公开(公告)日：2003-01-15

申请号：EP01927122.0

申请日：2001-04-17

申请人： SCHERING CORPORATION

发明人： POIRIER, Marc ,  WONG, Yee-Shing ,  WU, George, G.

IPC分类号： C07D221/16 ,  C07D213/79

CPC分类号： C07D213/79 ,  C07D221/16

摘要： A process is provided for preparing a compound having the formula (I) comprising: (a) reacting a compound having the formula (II) with an isocyanate having the formula R1NCO to produce a compound having the formula (III); (b) optionally hydrolyzing the compound of formula (III) to form an amide having the formula (IV); (c) reacting the compound of formula (III) or the amide of formula (IV) with a compound having the formula (V) in the presence of a strong base to produce a compound having the formula (VI); and (d) cyclizing the compound of formula (VI) to obtain the compound of formula (I), wherein R is H or Cl; M is selected from the group consisting of Li, Na, K, MgX, ZnRA, and Al(RA)2; RA is alkyl; X is halo; R1 is selected from the group consisting of alkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, and heterocycloalkylalkyl; and L is a leaving group. Also provided is a process for preparing a compound having the formula (VIII) comprising reacting a compound having the formula (II) with CO¿2? and a protonating agent to obtain the compound of formula (VIII), wherein M is selected from the group consisting of Li, Na, K, MgX, ZnR?A¿, and Al(RA)2, wherein RA is alkyl and X is halo.

公开(公告)号：EP2459525A1

公开(公告)日：2012-06-06

申请号：EP10737726.9

申请日：2010-07-27

申请人： Schering Corporation

发明人： TRAVERSE, John ,  LEONG, William, W. ,  MILLER, Steven, P. ,  ALBANEZE-WALKER, Jennifer ,  HUNTER, Thomas, J. ,  WANG, Lijun ,  LIAO, Hongbiao ,  ARASAPPAN, Ashok ,  TRZASKA, Scott, T. ,  SMITH, Randi, M. ,  LEKHAL, Azzeddine ,  BOGEN, Stephane, L. ,  KONG, Jianshe ,  BENNETT, Frank ,  NJOROGE, F., George ,  POIRIER, Marc ,  KUO, Shen-Chun ,  CHEN, Yonggang ,  MATTHEWS, Kenneth S. ,  DEMONCHAUX, Patrice ,  FERREIRA, Amadeo

IPC分类号： C07C315/00 ,  C07D209/52 ,  C07C237/02 ,  C07K5/06

CPC分类号： C07D209/52 ,  C07C51/353 ,  C07C67/04 ,  C07C237/04 ,  C07C315/02 ,  C07C315/04 ,  C07C317/28 ,  C07C319/14 ,  C07C319/20 ,  C07C2601/02 ,  C07C2601/14 ,  C07K5/0202 ,  C07K5/06034 ,  C07C323/53 ,  C07C317/44 ,  C07C57/03 ,  C07C69/533

摘要： Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed.

摘要翻译： 用于制备式I化合物的方法：式（I）。 公开了可用于制备式I化合物的中间体和用于制备所述中间体的方法。

公开(公告)号：EP1556358A2

公开(公告)日：2005-07-27

申请号：EP03799375.5

申请日：2003-10-01

申请人： SCHERING CORPORATION

发明人： CHEN, Frank, X. ,  WONG, Yee-Shing ,  ECKERT, Jeffrey, M. ,  ZOU, Nanfei ,  LIANG, Feng ,  KIM-MEADE, Agnes, S. ,  POIRIER, Marc ,  THIRUVENGADAM, Tiruvettipuram, K. ,  WU, George, G.

IPC分类号： C07D221/00

CPC分类号： C07D401/14 ,  C07D221/16

摘要： An enantioselective process for preparing intermediates useful in the preparation of the chiral tricyclic compound of formula (I), is disclosed.

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.