MANUFACTURING PROCESS FOR N-CARBOBENZYLOXY-L-GLUTAMIC ACID-ALPHA-CHOLINESTER SALT

摘要

The invention relates to manufacturing process for a halide or an organic sulfonate of N-carbobenzyl-L-glutamic acid- alpha -cholinester in high purification, which is useful as e.g. hypotensive drug. According to the prior art, undesired gamma -form byproduct is inevitably formed to be mingled with said alpha -form objective compound of which separation is difficult. It has been found that when using N-carbobenzyloxy- gamma -tert. butyl-L-glutamic acid-dicyclohexyl-ammonium salt readily available in high purification as starting material, reacting N, N-dimethyl-aminoethylchloride therewith to form N-carbobenzyloxy- gamma -tert. butyl-L-glutamic acid- alpha -dimethylaminoethyl ester which is quaternerized to form N-carbobenzyloxy- gamma -tert. butyl-L-glutamic acid- alpha -cholinester salt, which is subjected to mild salt treatment, the objective compound can be obtained in high purification.