Practical Asymmetric Synthesis of Sitagliptin Phosphate Monohydrate
2018
Haoling Gao | Jiangang Yu | Chengsheng Ge | Qun Jiang
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 Brø:nsted acid on tandem aza-Michael/hemiacetal reaction is researched in detail.
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