非对映体福提霉素1,2-环氧化物。1-脱氨基-2-脱氧福提霉素A和B以及1,2-二表福提霉素A和B的制备。

Diastereomeric fortimicin 1,2-epoxides. The preparation of the 1-deamino-2-deoxyfortimicins A and B and the 1,2-di-epi-fortimicins A and B.

作者信息

Martin J R, Johnson P, Tadanier J, Cirovic M, Stanaszek R S

出版信息

J Antibiot (Tokyo). 1982 Jan;35(1):46-57. doi: 10.7164/antibiotics.35.46.

DOI:10.7164/antibiotics.35.46

Abstract

The preparation of 1,2-anhydro-2',6'-di-N-benzyloxycarbonyl-1-deaminofortimicin B-4,5-carbamate (4) and its conversion to the two diastereomeric 2',6'-di-N-benzyloxycarbonyl-1-deamino-2-deoxy-1,2-epoxyfortimicin B-4,5-carbamates 7 and 13 are described. The olefin 4 was used for preparation of 1-deamino-2-deoxyfortimicin A (6d) while the beta-epoxide 13 was used for the preparation of 1,2-di-epi-fortimicin A (17b) and 2-amino-1-deamino-2-deoxy-1-hydroxyfortimicin A (19c). The in vitro antibacterial activities of 6d, 17b and 19c are reported.

摘要

描述了1,2-脱水-2',6'-二-N-苄氧羰基-1-脱氨福提米星B-4,5-氨基甲酸酯（4）的制备及其转化为两种非对映异构体的2',6'-二-N-苄氧羰基-1-脱氨基-2-脱氧-1,2-环氧福提米星B-4,5-氨基甲酸酯7和13的过程。烯烃4用于制备1-脱氨基-2-脱氧福提米星A（6d），而β-环氧化物13用于制备1,2-二表-福提米星A（17b）和2-氨基-1-脱氨基-2-脱氧-1-羟基福提米星A（19c）。报道了6d、17b和19c的体外抗菌活性。