| 摘要 |
<p>1377220 Preparation ofα-aminobenzylpenicillins E R SQUIBB & SONS Ine 14 Dec 1971 [29 Dec 1970] 58077/71 Heading C2C A process for the preparation of anα-aminobenzylpenicillin which is optionally substituted in the phenyl moiety comprises reacting a 6- arylidene-aminopenicillanic acid of general Formula I: wherein R represents a substituted or unsubstituted aryl group, with a phenylglycine N- carboxylic acid anhydride in a substantially anhydrous organic solvent followed by reaction with an arylamine. The aryl group R (and also the aryl group of the arylamine) may be a monocyclic or bicyclic carbocyclic aryl group, such as phenyl or naphthyl, which may be substituted with alkoxy, alkyl, phenyl, halogen or nitro groups. The phenyl group of the phenylglycine-N-carboxylic anhydride may be unsubstituted or bear a hydroxy, halogen or alkoxy group. Suitable solvents include halogenated hydrocarbons and the reaction may be carried out between 0‹ and 10‹ C. Reference has been directed by the Comptroller to Specifications 978,178, 902,703 and 873,049.</p> |
