Reduction of azides to primary amines in substrates bearing labile ester functionality. Synthesis of a PEG-solubilized, "Y"-shaped iminodiacetic acid reagent for preparation of folate-tethered drugs

被引：62

作者：

Lee, JW ^{[1
]}

Fuchs, PL ^{[1
]}

机构：

[1] Purdue Univ, Dept Chem, W Lafayette, IN 47907 USA

来源：

ORGANIC LETTERS | 1999年 / 1卷 / 02期

关键词：

D O I：

10.1021/ol9905248

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Anhydride 3 is a useful reagent for the synthesis of triply linked drug conjugates. Examples using paclitaxel are provided. Conversion of the azido moiety to a primary amine in the presence of substrates bearing labile ester functionality requires the use of a tin/mercaptan reducing system which includes methanol exchange equilibration to effect nitrogen-tin bond scission.

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页码：179 / 181

页数：3

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