Process for synthesis of eliglustat and intermediate compounds thereof
AssigneeZhejiang Ausun Pharmaceutical Co., Ltd.
InventorsYu Liu, Guanneng Yu, Zhiguo Zheng
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Abstract
A method for synthesis of Eliglustat and intermediate compounds thereof. Specifically, a method for synthesis of Eliglustat and pharmaceutically acceptable salts thereof, and further to intermediate compounds used in the method and a preparation method for the intermediate compounds. Compared with an existing synthesis method, the method for synthesis of Eliglustat of the present invention uses novel synthetic intermediates and synthesis steps, features ease of operation, high yield, good purity of intermediates and target products, etc., and facilitates industrial production.
Claims13
A process for preparation of Eliglustat and pharmaceutically acceptable salts thereof,
- the process comprising the following steps:
- (a-1) sulfonylation reaction of Compound V to give Compound VI,
- wherein R5 is hydrogen or hydroxy-protecting group, said hydroxy-protecting group is selected from alkyl, haloalkyl, aralkyl, alkoxyalkyl, allyl, acyl or silyl protective group,
- M is alkyl, aryl, substituted aryl or substituted alkyl,
- (a-2) reacting Compound VI with pyrrolidine to give Compound VII,
- (a-3) reducing Compound VII by catalytic hydrogenation with metal catalyst or reducing Compound VII with organophosphorus reagent, to give Compound VIII,
- (a-4) amidation reaction of Compound VIII with Compound IX to give Compound X,
- wherein R6 is selected from hydroxy, halogen or succimidyloxy,
- when R5 is hydrogen, Compound X is Eliglustat,
- or
- when R5 is hydroxy-protecting group, the following step is further carried out:
- (a-5) deprotecting Compound X to remove hydroxy-protecting group, to give Eliglustat
Dependencies are inferred from the claim text.