NEW METHOD FOR METHYLATION OF AMINES
NEW METHOD FOR METHYLATION OF AMINES
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DOI：
10.1021/jo00975a049
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发表时间：
1972-01-01
影响因子：
3.6
通讯作者：
HASSID, AI
中科院分区：
文献类型：
--
作者：
BORCH, RF;HASSID, AI
通过用甲醛和甲酸衍生物进行还原烷基化（Clarke-Eschweiler 方法2）将甲基引入伯胺或仲胺中已被证明是制备甲基化叔胺的有用方法。然而，在某些情况下，可能发生的多种副反应会产生复杂的混合物。 8 我们需要一种与目前正在研究的另一个问题相关的更温和的程序，再加上我们早期对氰基硼氢化物 (BHSCN-) 4 离子化学的兴趣，促使我们研究甲醛-氰基硼氢化物系统用于胺甲基化的可行性。我们在这里描述了一种温和有效的方法，用于以良好的产率合成高纯度的甲基化叔胺。
The introduction of methyl groups into a primary or secondary amine by reductive alkylation with form-aldehyde and formic acid derivatives (the Clarke-Eschweiler method2) has proved to be a useful method for the preparation of tertiary methylated amines. In some cases, however, complex mixtures have resulted from the multiplicity of side reactions which can occur. 8 Our need for a milder procedure in connection with another problem currently under investigation, cou-pled with our earlier interest in the chemistryof the cyanoborohydride (BHSCN-) 4 ion, led us to examine the feasibility of a formaldehyde-cyanoborohydride system for amine methylation. We describe here a mild and efficient method for thesynthesis of tertiary methylated amines ofhigh purity in good yield.