BINOL轴手性胍催化合成3,4-二氢嘧啶硫酮

Synthesis of 3,4-dihydropyrimidinthione catalyzed by BINOL axial chiral guanidine

以具有C 2轴手性结构的联萘酚酸骨架为原料,采用DCC-HOBt缩合法在联萘骨架上引入胍基,成功地合成了4个新型多氢键BINOL轴手性胍类催化剂,并将其成功应用于催化三组分不对称Biginelli反应。实验结果表明:在50℃条件下反应24 h,以甲醇为溶剂,1b作催化剂,取得了较好的收率(86%)。

Four novel BINOL axial chiral guanidine amides with multiple hydrogen bonds were synthesized by DCC-HOBt condensation from the enantiomeric structure of binapholic acid,and applied to three-component asymmetric Biginelli reaction.The results showed that the yield(86%)of the reaction were good when methanol was used as solvent and 1b as catalyst.