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1. Enantioselective synthesis of β-fluoroamines from β-amino alcohols: application to the synthesis of LY503430.

Author

Duthion B, Gomez Pardo D, and Cossy J

Subjects
Molecular Structure, Stereoisomerism, Amides chemical synthesis, Amines chemical synthesis, Amino Alcohols chemistry, Biphenyl Compounds chemical synthesis, Fluorine Compounds chemical synthesis
Abstract

N,N-Dialkyl-β-amino alcohols were enantiospecifically and regioselectively rearranged by using N,N-diethylaminosulfur trifluoride (DAST) to give optically active β-fluoroamines in excellent yields and enantiomeric excesses. This rearrangement was applied to the enantioselective synthesis of LY503430, a potential therapeutic agent for Parkinson's disease.

Published
2010
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