Abstract

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 (3 R )-7,8-difluoro-3-methyl-3,4‑dihydro-2 H -[1,4]benzoxazine was developed. How to Cite Gruzdev, D. A.; Vakarov, S. A.; Levit, G. L.; Krasnov, V. P. Chem. Heterocycl. Compd. 2014 , 49 , 1795. [ Khim. Geterotsikl. Soedin. 2013 , 1936.] For this article in the English edition see DOI 10.1007/s10593-014-1432-4

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