A solid-phase approach for the synthesis of α-aminoboronic acid peptides

被引：7

作者：

Daniels, Blake E. ^{[1
]}

Stivala, Craig E. ^{[1
]}

机构：

[1] Genentech Inc, Discovery Chem, 1 DNA Way, San Francisco, CA 94080 USA

来源：

RSC ADVANCES | 2018年 / 8卷 / 06期

关键词：

BORON-CONTAINING COMPOUNDS; BIOLOGICAL EVALUATION; MEDICINAL CHEMISTRY; POTENT INHIBITORS; AMINO-ACIDS; PROTEASOME; DESIGN; ESTERS; IDENTIFICATION; ANTIBACTERIAL;

D O I：

10.1039/c7ra13479g

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A solid-phase synthesis of alpha-aminoboronic acid peptides using a 1-glycerol polystyrene resin is described. Standard Fmoc solid-phase peptide chemistry is carried out to construct bortezomib and ixazomib. This approach eliminates the need for liquid-liquid extractions, silica gel column chromatography, and HPLC purifications, as products are isolated in high purity after direct cleavage from the resin.

引用

页码：3343 / 3347

页数：5

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