发明名称 6-HYDROXYALKYL-PENICILLINS
摘要 Penems of the formula I <CHEM> in which R is hydrogen or an organic radical, G is hydroxyloweralkyl and X is hydrogen, a pharmaceutically acceptable salt forming group or a metabolisable ester group, or a protecting group are disclosed. Process for their preparation involves reacting a compound II <CHEM> in which R1 and R2 are protected carboxy groups and Met is a thiophilic metal with a thiocarbonyl III S=C(Y)2 III in which Y is a leaving group, followed by removal of one of R1 and R2 to give a compound of formula I in which R is H together with its thione tautomer. Organic groups R can be introduced into the so-obtained compound by known methods. Alternatively the compound of formula I in which R is hydrogen can be made by intra-molecular cyclisation of the compound IV. <CHEM> G, Y and R2 being as previously defined. Various novel penems are also disclosed as well as three other processes for their preparation.
申请公布号 AU2167683(A) 申请公布日期 1984.06.07
申请号 AU19830021676 申请日期 1983.11.24
申请人 SCHERING CORP. 发明人 VIYYOOR MOOPIL GIRIJAVALLABHAN;ASHIT KUMAR GANGULY;PATRICK ANTHONY PINTO;RICHARD WILLIAM VERSACE;STUART WALTER MCCOMBIE
分类号 C07D499/897;A61K31/425;A61K31/43;A61P31/04;C07D205/08;C07D205/09;C07D233/54;C07D409/12;C07D499/00;C07D499/88;C07D499/893;C07F7/08;C07F7/18 主分类号 C07D499/897
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