Preparation methods of methyl-D3-amine and salts thereof
AssigneeSuzhou Zelgen Biopharmaceutical Co., Ltd.
InventorsXiaoyong Gao, Weidong Feng, Xiaojun Dai
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Abstract
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.
Claims7
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 or
- wherein 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.
A method for preparing (methyl-d3)amine or salts thereof, wherein, comprises:
- (a1) in an inert solvent and in the presence of a catalyst, reacting phthalimide with deuterated methanol 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.
Dependencies are inferred from the claim text.