| 摘要 |
<p>1492076 Penam compounds PFIZER Inc 18 Aug 1975 [5 Sept 1974] 34317/75 Heading C2C The invention comprises compounds of Formulae (III) and (V) [as well as acid addition salts of (III) when R=H], wherein R is H or an amino-protecting group excluding PhCH 2 CO and PhOCH 2 CO, R<SP>1</SP> is PhCH 2 or PhOCH 2 , and X is Cl, Br or C 1-4 alkoxy. In examples (III) (R=H) are conventionally tritylated, or (III) (R=Ph 3 C) are detritylated with acid; or the 3-carbamyl analogues are dehydrated to 3-CN; or (V) are treated with an alcohol to give (III) (R=H). (V) are prepared by treating the corresponding penicillin 2-amide or nitrile with PCl 5 /quinoline. (III) (R=Ph 3 C) are reacted with NaN 3 to give tetrazoles (I) (R=Ph 3 C), which in treatment with acid give tetrazoles (I) (R=H). The latter, on reaction with an acylating agent gives 6-acylamino-2,2-dimethyl-3-(5-tetrazolyl), penams (I : R = acyl ; Ia). Also prepared as a starting material is 6-tritylaminopenicillanic acid, triethylamine salt. Therapeutic compositions having antibacterial activity comprise the above acylamino compounds (Ia), and may be administered orally or parenterally.</p> |
