285136-76-7Relevant articles and documents
Highly enantioselective Biginelli reaction catalyzed by SPINOL-phosphoric acids
Xu, Fangxi,Huang, Dan,Lin, Xufeng,Wang, Yanguang
supporting information; experimental part, p. 4467 - 4470 (2012/07/14)
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.
Synthesis of enantiomerically pure 4-aryl-3,4-dihydropyrimidin-2(1H)-ones via enzymatic resolution: preparation of the antihypertensive agent (R)-SQ 32926
Schnell, Barbara,Strauss, Ulrike T.,Verdino, Petra,Faber, Kurt,Kappe, C. Oliver
, p. 1449 - 1453 (2007/10/03)
A practical and short synthesis of the enantiomerically pure dihydropyrimidone antihypertensive agent (R)-SQ 32926 has been developed. The key step in the synthesis is the enzymatic resolution of an N3-acetoxymethyl-activated dihydropyrimidone precursor b
