Solid-phase synthesis of 3,4-dihydro-1H-pyrimidine-2-ones using sodium benzenesulfinate as a traceless linker.
The facile preparation of 3,4-dihydropyrimidine-2-one derivatives with traceless solid-phase sulfone linker strategy is described. Key steps involved in the solid-phase synthetic procedure include (i) sulfinate acidification, (ii) condensation of urea or thiourea with aldehydes and sulfinic acid, and (iii) traceless product release via a one-pot cyclization-dehydration process. A library of 18 compounds was synthesized.
Li
Weiwei
W
Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543.
Lam
Yulin
Y
D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000737:chemistry*; D013441:Sulfinic Acids / Q000737:chemistry*
D011744:Pyrimidinones; D013441:Sulfinic Acids; C425152:benzenesulfinic acid