Total synthesis of γ-trifluoromethylated analogs of goniothalamin and their derivatives
Total synthesis of γ-trifluoromethylated analogs of goniothalamin and their derivatives
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DOI：
10.1016/j.jfluchem.2013.07.017
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发表时间：
2013-11-01
影响因子：
1.9
通讯作者：
Qing, Feng-Ling
中科院分区：
文献类型：
--
作者：
Chen, Jun-Ling;You, Zheng-Wei;Qing, Feng-Ling
本文报道了一种高效的手性γ-三氟甲基α，β-不饱和δ-内酯的合成方法，并成功地应用于γ-三氟甲基角噻草胺的合成。其关键步骤包括α-CF 3酰亚胺手性烯醇化钛的Evans-Aldol反应、Wittig烯化反应和内酯化反应。还研究了γ-三氟甲基化α，β-不饱和δ-内酯向一系列三氟甲基化苯乙烯基内酯的转化。(C)2013爱思唯尔有限公司版权所有。
An efficient method for the construction of chiral gamma-trifluoromethylated alpha,beta-unsaturated delta-lactone, a widely existing pharmacophore, has been developed and successfully applied for synthesis of gamma-trifluoromethylated goniothalamins. The key steps included Evans-Aldol reaction of chiral titanium enolate of alpha-CF3 imide, Wittig olefination and lactonization. The transformation of gamma-trifluoromethylated alpha,beta-unsaturated delta-lactone to a series of trifluoromethylated styryllactones was also investigated. (C) 2013 Elsevier B.V. All rights reserved.