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US3935193A Diacyl penicillins and methods for their production 失效
二酰基青霉素及其生产方法

Diacyl penicillins and methods for their production
摘要：
Novel diacyl penicillins of the formula ##EQU1## wherein R is alkyl, cycloalkyl, aryl, aralkyl, phenoxyalkyl, heterocyclic carboxyl excepting isoxazole carboxyl derivatives, or ##SPC1##In which benzene ring A may optionally be substituted andB represents a protective group for the amino group, and X is a protective group for the carboxyl group, are produced by reacting a benzyl penicillin ester of the formula ##EQU2## wherein X is as defined above, with a chlorinating agent in the presence of tertiary organic base to obtain an imide chloride group-incorporated compound of the formula ##EQU3## and then reacting the compound of the last-named formula with carboxylate of the formulaR-COOM (IV)wherein M is a metal atom, and R is as defined above.
摘要（中）：

式O CH2-C的新型二酰基青霉素O CH2-C ANGLE S ANGLE CH3 N-CH-CHC ANGLE |||CH3 RC ANGLE ||| O||| O = C-N --- CH-COOX（I）其中R 或烷基，环烷基，芳基，芳烷基，苯氧基烷基，除异恶唑羧基衍生物以外的杂环羧基，或其中任选取代的苯甲烯环，B表示氨基的保护基，X为羧基的保护基， 通过使式S ANGLE CH3 CH2-CO-NH-CH-CHC ANGLE |||CH3 O = C-N --- CH-COOX（II）的苄基青霉素酯反应制备，其中X如上定义， 在叔有机碱的存在下与氯化剂反应，得到式I化合物的酰亚胺氯化物基团化合物。ANGLE CH3 CH2-C = N-CH-CHC ANGLE ||| CH3 ClO = C-N --- CH-COOX，（III），然后使最后命名的化合物与式R-COOM（Ⅳ）的羧酸酯反应，其中M是金属原子，R如上定义。

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