An Efficient Method for the Preparation of Versatile Building Blocks: 1-Substituted 2,2-Dimethoxyethylamine Hydrochlorides

[摘要]：A novel method for the preparation of 1-substituted 2,2-dimethoxyethylamine hydrochlorides was developed. The method includes three highly efficient steps: (1) direct use of aqueous (MeO)(2)CHCHO for the preparation of N,O-acetal by condensation with Betti base without acidic catalyst; (2) regioselective alkylations of the NO-acetal with Grignard reagents; and (3) Pd/C catalytic hydrogenolyses of benzylamines in the presence of ClCH2CHCl2 to directly give the target products as crystalline amine hydrochlorides. The method reported is extremely convenient and highly efficient with wide substrate scopes.

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