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1. 发明授权

US07199240B2 Reductive alkylation of saturated cyclic amines 失效
标题翻译：饱和环胺的还原烷基化
公开(公告)号：US07199240B2
公开(公告)日：2007-04-03
申请号：US10726091
申请日：2003-12-02
申请人： James W. McManus , Bryan G. Kriel , Michael Stranberg
发明人： James W. McManus , Bryan G. Kriel , Michael Stranberg
IPC分类号： C07D401/06
CPC分类号： C07D213/38
摘要： Saturated cyclic amines (e.g., piperazines and piperidines) are reductively alkylated with an N-containing heteroaryl carbaldehyde using an alkylcarboxylic acid and a borohydride to obtain a product comprising an N-((N-containing heteroaryl)methyl)-substituted cyclic amine and one or more borane complexes thereof, after which the product is treated with a catalytic amount of a Pt or Pd catalyst in the presence of an alcohol to cleave the borane complex(es) and thereby afford the N-((N-containing heteroaryl)methyl)cyclic amine free of borane complex. Saturated cyclic amines are also reductively alkylated by adding an N-containing heteroaryl carbaldehyde and the amine to a tetrahydroborate salt-alkylcarboxylic acid-solvent admixture and aging the resulting reaction mixture to obtain an alkylated product substantially free of borane complex.
摘要翻译：使用烷基羧酸和硼氢化物将饱和环胺（例如哌嗪和哌啶）与含N杂芳基甲醛还原烷基化，得到包含N - （（N）杂芳基）甲基） - 取代的环状胺和一种或更多的硼烷配合物，之后在催化量的Pt或Pd催化剂的存在下，在醇的存在下处理产物以裂解硼烷络合物，由此得到N - （（N）杂芳基）甲基）环胺不含硼烷络合物。饱和环胺也通过将N含杂芳基甲醛和胺加入到四氢硼酸盐 - 烷基羧酸 - 溶剂混合物中进行还原烷基化，并使所得反应混合物老化，得到基本上不含硼烷络合物的烷基化产物。

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