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[抗肿瘤活性药物的研究。LXIII. 氨茴霉素及类似化合物。X. 11-苯基-5H-吡咯并[2,1-c][1,4]苯并二氮杂卓衍生物的合成]

[Research on agents with antineoplastic activity. LXIII. Anthramycin and analogous compounds. X. Synthesis of 11-phenyl-5H-pyrrolo[2,1-c] [1,4] benzodiazepine derivatives].

作者信息

Porretta G C, Scicchitano G, Filacchioni G, Scalzo M, Artico M

出版信息

Farmaco Sci. 1979 Oct;34(10):914-22.

PMID:510534
Abstract

Reaction between arolychlorides and 1-(2-aminobenzyl)-2-cyanopyrrole afforded the corresponding aroylamides, which were transformed by intramolecular cyclization into 11-aryl-3-cyano-5H-pyrrolo[2,1-c] [1,4] benzodiazepines. Hydrolysis of cyanoderivatives furnished the corresponding amides or acids depending on the reaction conditions. Decarboxylation and reduction of some derivatives to afford 11-aryl-5H-pyrrolo[2,1-c] [1,4] benzodiazepines and 11-aryl-3-cyano-10,11-dihydro-5H-pyrrolo[2,1-c] [1,4] benzodiazepines are described.

摘要

芳基氯与1-(2-氨基苄基)-2-氰基吡咯之间的反应生成了相应的芳酰胺,这些芳酰胺通过分子内环化转化为11-芳基-3-氰基-5H-吡咯并[2,1-c][1,4]苯并二氮杂䓬。氰基衍生物的水解根据反应条件提供相应的酰胺或酸。描述了一些衍生物的脱羧和还原反应,以得到11-芳基-5H-吡咯并[2,1-c][1,4]苯并二氮杂䓬和11-芳基-3-氰基-10,11-二氢-5H-吡咯并[2,1-c][1,4]苯并二氮杂䓬。

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