Synthetic applications of azolium ylides to a traceless solid-phase synthesis of 2-substituted azoles.
A new approach for the preparation of 2-substituted azole libraries using a polystyrene-carbamyl chloride resin in a traceless fashion is described. Azole substrates II are assembled in a one-pot condensation reaction of azoles and aldehydes with a resin-bound carbamyl chloride. Treatment of the azolyl-carbamate II with boron trifluoride etherate under thermal or microwave-assisted solvolysis conditions afforded 2-substituted azoles. [reaction: see text]
Deng
Yijun
Y
Drug Discovery, Johnson & Johnson Pharmaceutical Research & Development, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
Hlasta
Dennis J
DJ
D001393:Azoles / Q000138:chemical synthesis* / Q000737:chemistry; D007202:Indicators and Reagents; D008958:Models, Molecular; D008968:Molecular Conformation
D001393:Azoles; D007202:Indicators and Reagents