摘要

A domino reaction, based on an organocatalysed sulfa-Michael/Michael sequence, is demonstrated as being useful for the asymmetric synthesis of spiro[pyrazolone-4,3'-tetrahydrothiophenes] bearing three consecutive stereocentres. This new class of spirocyclic compounds has been synthesised in good yield and fairly good diastereo- and enantioselectivity by reacting alpha,beta-unsaturated pyrazolones and tert-butyl (E)-4-mercapto-2-butenoate in the presence of a readily available secondary amine thiourea derived from (R,R)-1,2-diphenylethylenediamine.

  • 出版日期2017-4