Asymmetric synthesis of optically active α-substituted α-amino-H-phosphinates through resolution of 1,1-diethoxyethyl(aminomethyl)phosphinates |
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Authors: | Terumitsu Haruki Takehiro Yamagishi Tsutomu Yokomatsu |
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Institution: | aSchool of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan |
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Abstract: | Both enantiomers of 1,1-diethoxyethyl(aminomethyl)phosphinates were prepared through chromatographic separation of a diastereomeric mixture derived from (S)-phenylethylamine and 1,1-diethoxyethyl-H-phosphinate. The individual enantiomer was transformed into α-substituted α-amino-H-phosphinate with high enantiomeric purity by a highly diastereoselective alkylation at the α-carbon on the basis of our previously developed method. |
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