| 摘要 |
1,268,631. N-Acylating 6-amino-penicillin. YEDA RESEARCH & DEVELOPMENT CO. Ltd. 17 March, 1969 [21 March, 1968], No. 13840/68. Heading C2A. [Also in Division C3] A process for N-acylating 6-amino-penicillanic acid comprises contacting a solution of the said acid or a salt, ester, amide or other functional derivative thereof with a solid acylating polymer insoluble in the solution and comprising recurring groups of formula -BRCO wherein RCO is an organic acyl group and B is an activated group, separating solid material from the solution and recovering from the solution the corresponding N-acylated penicillin derivative, optionally as a non-toxic salt. The polymer consists of a series of repeating groups of formula wherein A is the repeating unit of a synthetic or natural polymeric chain. It is prepared by acylating a suitable polymer e.g. poly-(4-hydroxy-3-nitro)-styrene, or a polymer of N- hydroxy-maleimide which may be co-polymerized with ethylene (see Division C3). The inventive reaction may be performed in aqueous or non-aqueous solution and the product recovered by evaporation, extraction or lyophilization. Examples are given for preparing benzyl-; 2,6- dimethoxyphenyl-, 3 - (2 - chlorophenyl) - 5 - methyl-4-isoxazoloyl-; phenoxyethyl-; and carboxy benzyl-penicillins. |
