title: Highly enantioselective Biginelli reaction catalyzed by SPINOL-phosphoric acids.
abstract: A highly enantioselective Biginelli reaction promoted by chiral spirocyclic SPINOL-phosphoric acids has been developed. Under the optimized conditions with 5 mol% catalyst loading, a wide range of optically active dihydropyrimidinethiones (DHPMs) were obtained in high yields (up to 98%) with good to excellent enantioselectivities (up to 99% ee). The synthetic utility of this method was demonstrated by the synthesis of chiral precursors of three drugs, including (S)-Monastrol, (S)-L-771688 and (S)-SQ 32926.
authors.affiliation: Department of Chemistry, Zhejiang University, Hangzhou 310027, China.
authors.forename: Fangxi
authors.initials: F
authors.lastname: Xu
authors.forename: Dan
authors.initials: D
authors.lastname: Huang
authors.forename: Xufeng
authors.initials: X
authors.lastname: Lin
authors.forename: Yanguang
authors.initials: Y
authors.lastname: Wang