Practical Asymmetric Synthesis of Sitagliptin Phosphate Monohydrate
Copyright policy )Practical Asymmetric Synthesis of Sitagliptin Phosphate Monohydrate
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.
- Quzhou University China (People's Republic of)
- Zhejiang University of Technology China (People's Republic of)
- Zhejiang University of Science and Technology China (People's Republic of)
QD241-441, Molecular Structure, asymmetric synthesis, Sitagliptin Phosphate, sitagliptin phosphate monohydrate, Organic chemistry, Stereoisomerism, aza-Michael/hemiacetal reaction, Article, Catalysis
QD241-441, Molecular Structure, asymmetric synthesis, Sitagliptin Phosphate, sitagliptin phosphate monohydrate, Organic chemistry, Stereoisomerism, aza-Michael/hemiacetal reaction, Article, Catalysis
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