Intermediates for preparing 2-(substituted-dibenzofuranyl and
申请人:Merck & Co., Inc.
公开号:US05151512A1
公开(公告)日:1992-09-29
Carbapenem intermediates having the formula: ##STR1## where Z is; ##STR2## M is a removable protecting group for carboxy and P' is a removable protecting group for hydroxy are useful intermediates for preparing antibacterial agents, especially with respect to activity against methicillin resistant Staphylococcus aureus (MRSA).
碳青霉烯中间体具有以下化学式:##STR1## 其中 Z 为;##STR2## M 是羧基的可去保护基,P' 是羟基的可去保护基,这些中间体对于制备抗菌剂特别是针对耐甲氧西林金黄色葡萄球菌(MRSA)的活性是有用的。
2-(substituted-dibenzofuranyl and dibenzothienyl) carbapenem
申请人:Merck & Co., Inc.
公开号:US05240920A1
公开(公告)日:1993-08-31
Carbapenems having the formula: ##STR1## where X is O or S(O).sub.0-2 ; are useful antibacterial agents, especially with respect to activity against methicillin resistant Staphylococcus aureus (MRSA).
Intermediates for preparing 2-(substituted-dibenzo-furanyl and
申请人:Merck & Co., Inc.
公开号:US05132420A1
公开(公告)日:1992-07-21
Carbapenem intermediates having the formula: ##STR1## where Z is ##STR2## M is a removable protecting group for carboxy and P' is a removable protecting group for hydroxy, are useful intermediates for preparing antibacterial agents, especially with respect to activity against methicillin resistant Staphylococcus aureus (MRSA).
具有公式:##STR1## 的碳青霉烯中间体,其中 Z 是 ##STR2##,M 是羧基的可去保护基,P' 是羟基的可去保护基,是制备抗菌剂的有用中间体,特别是对甲氧西林耐药金黄色葡萄球菌(MRSA)的活性。
3-aryl of heteroaryl-7-heteroaralkylamido cephalosporin compounds,
申请人:Merck & Co. Inc.
公开号:US05455239A1
公开(公告)日:1995-10-03
A compound of the formula I is disclosed. ##STR1## R.sup.13 represents hydrogen, NH.sub.2, C1-4 alkyl, C1-4 alkylamino or di(C1-4) alkylamino-; Y represents CH or N; Y" represents (a) CR.sup.y' R.sup.z' with R.sup.y' and R.sup.z' hydrogen, C1-6 alkyl, C.sub.3-8 cycloalkyl or C.sub.1-6 alkyl substituted with C.sub.3-8 cycloalkyl, or (b) N substituted with OR.sup.14 with R.sup.14 representing H, C.sub.1-4 alkyl or C.sub.1-4 alkyl substituted with COOH. Ar represents: ##STR2## One of R.sup.1 and R.sup.2 independently represent H, W as defined below or one of the groups (a) through (d) below, and the other represents H or W. Pharmaceutical compositions and methods of use are also included.
Carbapenems having the formula:
are prepared by a novel reaction of a readily accessible carbapenem intermediate and an organostannane. The reaction, which is mediated by a palladium compound and, optionally, a phosphine ligand, proceeds at remarkably mild temperatures in reproducibly good yields.