Preparation methods of methyl-D3-amine and salts thereof

摘要

Preparation methods of methyl-d3-amine and salts thereof are provided, which contain the following steps: (i) nitromethane is subjected to react with deuterium oxide in the present of bases and phase-transfer catalysts to form nitromethane-d3, which is subsequently subjected to reduction in an inert solvent to form methyl-d3-amine, and optionally, methyl-d3-amine reacts subsequently with acids to form salts of methyl-d3-amine; or (ii) N-(1,1,1-trideuteriomethyl)phthalimide is subjected to react with acids to form salts of methyl-d3-amine. The present methods are easy, high efficient, and low cost.

主权项

1. A method for preparing (methyl-d3)amine or salts thereof, wherein, comprises:
(a2) in an inert solvent, reacting an alkali metal salt of phthalimide with compound A, wherein, Z is CH3, O-CD3 orwherein R is methyl, nitro or halogen to form N-(methyl-d3)phthalimide; step (b) reacting N-(methyl-d3)phthalimide with an acid to form the salt of (methyl-d3)amine; and optional step (c): reacting the salt of (methyl-d3)amine with a base to form (methyl-d3)amine.