N-Tosyl-(S)-Prolyl Chloride in Kinetic Resolution of Racemic Heterocyclic Amines
N-Tosyl-(S)-Prolyl Chloride in Kinetic Resolution of Racemic Heterocyclic Amines
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DOI：
10.1007/s10593-014-1432-4
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发表时间：
2014-03-01
影响因子：
1.5
通讯作者：
Krasnov, V. P.
中科院分区：
文献类型：
--
作者：
Gruzdev, D. A.;Vakarov, S. A.;Krasnov, V. P.
研究了N-对甲苯磺酰基-（S）-脯氨酰氯酰化拆分外消旋杂环胺的动力学。它被确定，芳香胺的外消旋混合物可以被解决与高效率，而2-和3-甲基哌啶的酰化反应发生低非对映选择性。研究了一种制备光学纯的（3R）-7，8-二氟-3-甲基-3，4-二氢-2H-[1，4]苯并恶嗪的方法。
The kinetic resolution of racemic heterocyclic amines via acylation with N-tosyl-(S)-prolyl chloride was systematically investigated. It was established that racemic mixtures of aromatic amines could be resolved with high efficiency, while the acylation of 2- and 3-methylpiperidines occurred with low diastereoselectivity. A method for the preparation of enantiomerically pure (3R)-7,8-difluoro-3-methyl-3,4-dihydro-2H-[1,4]benzoxazine was developed.