Synthetic method for telotristat ethyl intermediate

Abstract

The present invention provides a method for synthesizing the intermediate of compound telostat ethyl ester of formula (1). The compound of formula (1) is finally prepared by using formula (2) as the starting raw material through reductase reduction reaction. Telostat ethyl ester intermediate: Compared with the complex synthesis process and high synthesis cost of the telostat ethyl ester intermediate in the prior art, the synthetic method of the present invention is simple and easy, with lower cost and higher yield, and the product Good quality, suitable for large-scale industrial production.

Description

technical field [0001] The invention relates to a synthesis method of a telostat ethyl ester intermediate, belonging to the technical field of medicine synthesis. Background technique [0002] Telostat ethyl ester (common name: Telotristat ethyl, trade name Xermelo), chemical name: (S)-2-amino-3-(4-(2-amino-6-((R)-1- (4-Chloro-2-(3-methyl-1H-pyrrol-1-yl)phenyl)-trifluoroethoxy)pyridin-4-yl)phenyl)propanoic acid ethyl ester. The molecular weight of terolustat ethyl ester: 574.99; CAS registration number: 1033805-22-9; the structural formula is shown in formula 1: [0003] [0004] Formula 1 [0005] Telostat ethyl ester was developed by Lexicon Pharmaceuticals. On February 28, 2017, a drug for the treatment of carcinoid syndrome (carcinoid syndrome) approved in the United States, Telotristat (terostat ethyl ester) is an inhibitor of tryptophan hydroxylase, which inhibits the cause of carcinoid syndrome Synthesis of serotonin. [0006] prior art literature [0007] No...

AI Technical Summary

Problems solved by technology

[0009] In the prior art, the synthesis process of terolustat ethyl ester intermediate is often more complicated, the cost is higher, and there are also defects of low product yield and poor quality, which cannot be suitable for industrialized large-scale production

Images