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：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：EP2051963A1

公开(公告)日：2009-04-29

申请号：EP07837002.0

申请日：2007-08-17

申请人： Schering Corporation

发明人： CHEN, Frank, Xing ,  TAMAREZ, Maria, M. ,  XIE, Ji

IPC分类号： C07D211/22

CPC分类号： C07D211/22

摘要： The present invention provides a method of resolving piperdin-yl- alkylene-alcohols, in high yield at high enantiomeric purity, for example 2- piperidin-2-yl-ethanol.

公开(公告)号：EP1131313A1

公开(公告)日：2001-09-12

申请号：EP99958771.0

申请日：1999-11-18

申请人： SCHERING CORPORATION

发明人： KUO, Shen-Chun ,  BERNARD, Charles, F. ,  CHEN, Frank, Xing ,  HOU, Donald ,  KIM-MEADE, Agnes, S. ,  WU, George, G.

IPC分类号： C07D401/04 ,  C07B53/00

CPC分类号： C07D401/04 ,  C07D401/14 ,  Y02P20/55

摘要： Disclosed is a process for preparing a compound of formula (I) wherein X?1, X2, X3, X4 and X5¿ are independently selected from the group consisting of H, halo, alkyl, alkoxy, aryl, and aryloxy, and R is a protecting group, in which a compound having formula (II) wherein X?1, X2, X3, X4 and X5¿ are as defined above, is treated with the following, in any sequence: (a) a non-nucleophilic strong base; (b) a chiral amino alcohol; and (c) a compound having formula (V) wherein L is a leaving group and R is as defined above. The compounds made by this process are useful intermediates for preparing compounds that are inhibitors of farnesyl protein transferase.

公开(公告)号：EP2051963B1

公开(公告)日：2012-05-16

申请号：EP07837002.0

申请日：2007-08-17

申请人： Schering Corporation

发明人： CHEN, Frank, Xing ,  TAMAREZ, Maria, M. ,  XIE, Ji

IPC分类号： C07D211/22

CPC分类号： C07D211/22

摘要： The present invention provides a method of resolving piperdin-yl- alkylene-alcohols, in high yield at high enantiomeric purity, for example 2- piperidin-2-yl-ethanol.

公开(公告)号：EP2234971A1

公开(公告)日：2010-10-06

申请号：EP08862706.2

申请日：2008-12-16

申请人： Schering Corporation

发明人： CHEN, Frank, Xing ,  CUTARELLI, Timothy, D. ,  FU, Xiaoyong ,  LIANG, Xian ,  MCALLISTER, Timothy, L. ,  ORR, Robert, K. ,  YIN, Jianguo ,  YONG, Kelvin, H. ,  ZHU, Man

IPC分类号： C07D211/44 ,  C07D239/42 ,  C07D413/14 ,  C07D295/205 ,  A61K31/497

CPC分类号： C07D413/14 ,  C07D211/44 ,  C07D239/42 ,  C07D295/205

摘要： The present invention relates to novel processes for the preparation of the compound of the Formula A45: [Chemical formula should be inserted here as it appears in the paper abstract.] or a physiologically acceptable salt, solvate or prodrug thereof, which has utility, for example, as a pharmaceutically active compound with CXCR3 antagonist activity, and to novel intermediates useful in the synthesis thereof.

公开(公告)号：EP1131313B1

公开(公告)日：2003-02-26

申请号：EP99958771.0

申请日：1999-11-18

申请人： SCHERING CORPORATION

发明人： KUO, Shen-Chun ,  BERNARD, Charles, F. ,  CHEN, Frank, Xing ,  HOU, Donald ,  KIM-MEADE, Agnes, S. ,  WU, George, G.

IPC分类号： C07D401/04 ,  C07B53/00

CPC分类号： C07D401/04 ,  C07D401/14 ,  Y02P20/55

摘要： Disclosed is a process for preparing a compound of formula (I) wherein X?1, X2, X3, X4 and X5¿ are independently selected from the group consisting of H, halo, alkyl, alkoxy, aryl, and aryloxy, and R is a protecting group, in which a compound having formula (II) wherein X?1, X2, X3, X4 and X5¿ are as defined above, is treated with the following, in any sequence: (a) a non-nucleophilic strong base; (b) a chiral amino alcohol; and (c) a compound having formula (V) wherein L is a leaving group and R is as defined above. The compounds made by this process are useful intermediates for preparing compounds that are inhibitors of farnesyl protein transferase.