PROCESS FOR THE PREPARATION OF N-ACYL BETA-AMINOALDEHYDES
This invention relates to a process for the preparation of enantiomerically enriched N--acyl ?-aminoaldehydes. In particular it relates to asymmetric hydrogenation of N-acyl enamides.
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Page/Page column 24-25
(2010/11/08)
Lipase-catalyzed resolution of chiral 1,3-amino alcohols: application in the asymmetric synthesis of (S)-dapoxetine
The enzymatic resolution of 3-amino-3-phenylpropan-1-ol derivatives has been studied through acylation processes. Candida antarctica lipase A (CAL-A) has been identified as the best biocatalyst for the transesterification reaction of 3-amino-3-phenyl-1-tert-butyldimethylsilyloxy-propan-1-ol using ethyl methoxyacetate as acylating agent and tert-butyl methyl ether as solvent. This enzymatic study has allowed us to obtain a valuable intermediate for the production of (S)-dapoxetine, which has been synthesized in good overall yield and high enantiomeric excess.
The reaction of oxetanes with acrylonitrile and benzonitrile in the presence of concentrated sulfuric acid leads to the formation of the corresponding 5,6-dihydro-1,3-oxazines.
Pavel', T. M.
p. 157 - 159
(2007/10/02)
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