Improved syntheses of α-BOC-aminoketones from α-BOC-amino-Weinreb amides using a pre-deprotonation protocol
Improved syntheses of α-BOC-aminoketones from α-BOC-amino-Weinreb amides using a pre-deprotonation protocol
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DOI：
10.1016/s0040-4039(02)02031-2
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发表时间：
2002-11-11
影响因子：
1.8
通讯作者：
Armstrong, JD
中科院分区：
文献类型：
--
作者：
Liu, J;Ikemoto, N;Armstrong, JD
开发了一种从含有可交换氨基质子的α-BOC-氨基Weinreb酰胺以良好收率制备α-BOC-氨基酮的一般方法。通过首先使用1当量将该氨基去质子化，简单的烷基格氏碱，仅需要化学计量的量，而不是大量过量的亲核试剂来制备酮。因此，该方法运行起来更经济，并且纯化更容易。(C)2002爱思唯尔科技有限公司。保留所有权利。
A general procedure was developed to prepare alpha-BOC-aminoketones in good yields from alpha-BOC-amino Weinreb amides containing an exchangeable amino proton. By first deprotonating this amino group using 1 equiv. of a simple alkyl Grignard base, only a stoichiometric amount, rather than a large excess, of the nucleophile was needed to prepare the ketone. This procedure is therefore more economical to run and the purification is easier. (C) 2002 Elsevier Science Ltd. All rights reserved.