Cheng K F, Yip C S, Yeung H W, Kong Y C
Experientia. 1979 May 15;35(5):571-2. doi: 10.1007/BF01960323.
Leonurine (1) is the uterotonic principle of Leonurus artemisia. We have developed a simple, high-yield synthetic procedure of 1 that is adaptable to large scale preparation. The synthesis involves the condensation of syringic acid and 4-guanidino-1-butanol hydrochloride in the presence of DDC using 1:1 HMPT-ether as solvent. The synthetic leonurine showed uterotonic activity in vivo and in vitro.
益母草碱(1)是益母草的子宫收缩活性成分。我们已经开发出一种简单、高产率的合成方法来制备1,该方法适用于大规模制备。合成过程包括在DDC存在下,以1:1的HMPT - 醚为溶剂,使丁香酸与4 - 胍基 - 1 - 丁醇盐酸盐缩合。合成的益母草碱在体内和体外均表现出子宫收缩活性。