Sheng Tao, Ma Caiyun, Zhang Guangyan, Pan Xuan, Liu Zhanzhu
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, People's Republic of China.
J Nat Prod. 2022 Apr 22;85(4):1128-1133. doi: 10.1021/acs.jnatprod.2c00069. Epub 2022 Mar 3.
The first total synthesis of griseofamine B is described starting from l-4-bromo tryptophan methyl ester hydrochloride via five steps and in 18% overall yield. Its three stereoisomers were also synthesized following the same procedure with the yields of 5%, 19%, and 5%, respectively. antibacterial activities were also evaluated. All four compounds exhibited less potent activity than griseofamine A.
描述了从L-4-溴色氨酸甲酯盐酸盐开始，经五步反应，以18%的总收率首次全合成灰黄霉素B。还按照相同程序合成了其三种立体异构体，收率分别为5%、19%和5%。还评估了抗菌活性。所有四种化合物的活性均低于灰黄霉素A。
