Highly stereoselective synthesis of non-racemic 3-substituted dihydro-benzo[de]isoquinolinones via an addition-cyclization-substitution method

摘要

Substituted dihydrobenzo[de]isoquinolinones were synthesized via diastereoselective addition of Grignard reagents to the N-tert-butylsulfinylimine derived from 1,8-naphthaldehydic methyl ester, followed by cyclization and substitution at the sulfur atom. The products were obtained in 25-98% yield and with enantiomeric excess of 46-99%. (C) 2020 The Authors. Published by Elsevier Ltd.