Manufacturing process for n-carbobenzyloxy-l-glutamic...

C - Chemistry – Metallurgy – 07 – C

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260/468.1

C07C 125/065 (1985.01)

Patent

CA 1220219

ABSTRACT OF THE DISCLOSURE The invention relates to manufacturing process for a halide or an organic sulfonate of N-carbobenzyl- L-glutamic acid-?-cholinester in high purification, which is useful as e.g. hypotensive drug. According to the prior art, undesired ?-form byproduct is inevitably formed to be mingled with said ?-form objective compound of which separation is difficult. It has been found that when using N-carbobenzyloxy-?- 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-?-tert. butyl-L-glutamic acid-?-dimethylaminoethyl ester which is quaternerized to form N-carbobenzyloxy-?-tert. butyl-L-glutamic acid-?-cholinester salt, which is subjected to mild salt treatement, the objective compound can be obtained in high purification.

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