A versatile method for the preparation of 2,2-disubstituted morpholine analogues

被引:19
作者
Takemoto, T [1 ]
Iio, Y [1 ]
Nishi, T [1 ]
机构
[1] Sankyo Co Ltd, Med Chem Res Labs, Shinagawa Ku, Tokyo 1408710, Japan
关键词
D O I
10.1016/S0040-4039(00)00016-2
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
We describe a versatile synthetic method for the preparation of 2,2-disubstituted morpholine analogues. Iodoetherification of 1,1-disubstituted olefin with N-Boc-aminoethanol using NIS proceeded smoothly in a regioselective manner and the following cyclization was accomplished in good yield. We successfully applied this method for the preparation of the key intermediate 2 of tachykinin receptor antagonist. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1785 / 1788
页数:4
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