公开(公告)号：EP1328523A2

公开(公告)日：2003-07-23

申请号：EP01987748.9

申请日：2001-10-12

申请人： Bristol-Myers Squibb Company

发明人： POLNIASZEK, Richard, P. ,  WANG, Xuebao ,  THOTTATHIL, John, K. ,  DENZEL, Theodor

IPC分类号： C07D413/12

CPC分类号： C07D413/12 ,  C07D261/16 ,  C07F5/025

摘要： Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates thereof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endothelin antagonists useful, inter alia, for the treatment of hypertension.

公开(公告)号：EP1051419A1

公开(公告)日：2000-11-15

申请号：EP98963113.0

申请日：1998-12-11

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： KRONENTHAL, David, R. ,  DENZEL, Theodor ,  CHEN, Bang-Chi ,  SIMPSON, James, H. ,  DESHPANDE, Rajendra, P.

IPC分类号： C07D471/02 ,  C07D513/04

CPC分类号： C07D513/04 ,  C07D223/12

摘要： Acylmercaptoalkanoylamino lactam esters or acids are converted to the corresponding mercaptoalkanoylamino lactam ester or acid under basic conditions by including an agent which minimizes the amount of disulfides. Suitable agents are bismercaptans, phosphine or phosphite reducing agents, zinc metal powder, and sodium hydrosulfite. Such agents are also employed in the recrystallization and reprocessing of the mercaptoalkanoylamino lactam acids.