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Practical Asymmetric Synthesis of Sitagliptin Phosphate Monohydrate

Haoling Gao, Jiangang Yu, Chengsheng Ge, Qun Jiang

Molecules. 2018 Jun 13;23(6):1440.

PMID: 29899310

Abstract:

Optically pure sitagliptin phosphate monohydrate is efficiently and practically synthesized through a chiral hemiacetal as the key intermediate in 54% overall yield starting from (E)-4-(2,4,5-trifluorophenyl)but-2-enal and N-boc-protected hydroxylamine. The chiral hemiacetal fragment is constructed by a tandem aza-Michael/hemiacetal reaction catalyzed by an organocatalyst and the influence of acidity of Brønsted acid on tandem aza-Michael/hemiacetal reaction is researched in detail.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP654671779 Sitagliptin phosphate Sitagliptin phosphate 654671-77-9 Price
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