SYNTHESIS OF 16-DECARBOXY-16-HYDROXYMETHYL AMPHOTERICIN-B - A NOVEL ANTIFUNGAL AGENT

被引：12

作者：

DRIVER, MJ ^{[1
]}

GREENLESS, AR ^{[1
]}

MACLACHLAN, WS ^{[1
]}

MACPHERSON, DT ^{[1
]}

TAYLOR, AW ^{[1
]}

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT,GREAT BURGH,YEW TREE BOTTOM RD,EPSOM KT18 5XQ,SURREY,ENGLAND

来源：

TETRAHEDRON LETTERS | 1992年 / 33卷 / 30期

关键词：

NOVEL POLYENE ANTIBIOTIC; AMPHOTERICIN-B DERIVATIZATION; ANTIFUNGAL AGENT; REDUCTION; N-FMOC PROTECTION;

D O I：

10.1016/S0040-4039(00)74259-6

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The synthesis of the novel polyene, 16-decarboxy-16-hydroxymethyl amphotericin B 5, the first monofunctionalised amphotericin B derivative without a carbonyl containing substituent in the C-16 position, is described. This primary alcohol 5, which shows negligible nephrotoxicity while maintaining good antifungal activity, was obtained via reduction of the novel N-Fmoc protected mycosamine containing derivative 8.

引用

页码：4357 / 4360

页数：4

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