m-甲基-8β-O-肉桂酰基-goniotriol的不对称合成

Asymmetric synthesis of m-methyl-8β-O-cinnamoyl goniotriol

目的 为了研究哥纳香醇甲的构效关系和寻找更高抗肿瘤活性的化合物。方法 以α -D -葡庚糖酸内酯为原料 ,以 9步反应 ,不对称选择性地合成了m -甲基 - 8β -O -肉桂酰基 -goniotriol,总收率为 5 .7% ,并经MTT法检测了它们的抗肿瘤活性。结果 合成了m -甲基 - 8β -O -肉桂酰基 -goniotriol及其 3个中间体 ,均为新化合物。 结论

Objective To investigate the relationship tetween structure and activity of Howiinol A and to find more potent antitumor compounds.Methods m-Methyl-8β-cinnamoyl goniotriol was asymmetrically synthesized in nine steps from α-D-glucoheptonic δ-lactone.The antitumor activities of m-Methyl-O-cinnamoyl-goniotriol and its intermediates were screened by MTT methods.Results m-Methyl-8β-cinnamoyl goniotriol and its intermediates were synthesized.Some of them are new compounds.The overall yield of m-Methyl-8β-O-cinnamoyl-goniotriol was 5.7%.Conclusions Pharmacological tests show that most of them possess activities againt tumor cells in vitro.