REDUCTIVE ALKYLATION ON A SOLID-PHASE - SYNTHESIS OF A PIPERAZINEDIONE COMBINATORIAL LIBRARY

被引：158

作者：

GORDON, DW ^{[1
]}

STEELE, J ^{[1
]}

机构：

[1] PFIZER LTD,CENT RES,DEPT DISCOVERY CHEM,SANDWICH CT13 9NJ,KENT,ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 01期

关键词：

D O I：

10.1016/0960-894X(94)00455-O

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of a prototype trisubstituted piperazinedione combinatorial library of 1,000 compounds has been achieved from three precursor sets - two sets of ten a-amino acids and one set of ten aldehydes. A sodium triacetoxyborohydride-mediated reductive alkylation was crucial to the success of the multi-step synthesis on resin. This protocol represents a new method to augment compound files rapidly with novel heterocyclic entities for high-speed screening.

引用

页码：47 / 50

页数：4

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