A new one-pot method for the synthesis of α-siloxyamides from aldehydes or ketones and its application to the synthesis of (-)-bestatin
A new one-pot method for the synthesis of α-siloxyamides from aldehydes or ketones and its application to the synthesis of (-)-bestatin
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DOI：
10.1021/ol006816m
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发表时间：
2000-12-28
期刊：
影响因子：
5.2
通讯作者：
Shibuya, M
中科院分区：
文献类型：
--
作者：
Nemoto, H;Ma, RJ;Shibuya, M
[图表]描述了一种合成 α-甲硅烷氧基酰胺的新一锅法。将三种底物 H-C(CN)(2)O-SiMe(2)t-Bu、醛或酮以及伯胺或仲胺简单地在乙腈或乙醚中混合一份；在许多情况下，α-甲硅烷氧基酰胺可以在短时间内以优异的产率获得。作为我们方法的演示，进行了 (-)-bestatin 的合成。
[GRAPHICS]A new one pot method for the synthesis of alpha -siloxyamides is described. The three substrates, H-C(CN)(2)O-SiMe(2)t-Bu, aldehydes or ketones, and primary or secondary amines, are simply mixed in one portion in acetonitrile or ether; the a-siloxyamides are obtained within short peroids in excellent yields in many cases. As a demonstration of our method, the synthesis of (-)-bestatin was carried out.