Preparation and improved stability of N-Boc-α-amino-5-acyl Meldrum's acids, a versatile class of building blocks for combinatorial chemistry

被引：23

作者：

Raillard, SP ^{[1
]}

Chen, WW ^{[1
]}

Sullivan, E ^{[1
]}

Bajjalieh, W ^{[1
]}

Bhandari, A ^{[1
]}

Baer, TA ^{[1
]}

机构：

[1] Affymax Inc, Palo Alto, CA 94304 USA

来源：

JOURNAL OF COMBINATORIAL CHEMISTRY | 2002年 / 4卷 / 05期

关键词：

D O I：

10.1021/cc0200033

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

The preparation of novel N-Boc-alpha-amino-5-acyl Meldrum's acids is described. The synthetic inaccessibility and instability of several of these products have led to the development of a protocol that allows the synthesis of their corresponding 4-(dimethylamino)pyridine (DMAP) salts (5-AMA-DMAP's), which exhibit superior stability compared to that of the free 5-AMA. A simple and expedient ion-exchange method was developed for the quantitative removal of DMAP to liberate the synthetically useful DMAP-free form when needed.

引用

页码：470 / 474

页数：5

共 18 条

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