Wissner A, Kohler C A, Goldstein B M
J Med Chem. 1985 Sep;28(9):1365-7. doi: 10.1021/jm00147a045.
An analogue of platelet activating factor (PAF) in which the phosphate moiety has been replaced with a sulfonylbismethylene group has been prepared. A key step in the synthetic sequence is the preparation of 4-[[3-(dimethylamino)propyl]thio]-1-(hexadecyloxy)-2-butanol via a one-pot reaction involving a sequential Michael addition and reduction. In comparison to racemic C16-PAF, 8 showed no platelet aggregating activity and substantially reduced hypotensive activity.
已制备出一种血小板活化因子（PAF）类似物，其中磷酸部分已被磺酰双亚甲基基团取代。合成序列中的关键步骤是通过一锅法反应制备4-[[3-(二甲氨基)丙基]硫基]-1-(十六烷氧基)-2-丁醇，该反应涉及连续的迈克尔加成和还原反应。与外消旋C16-PAF相比，8没有显示出血小板聚集活性，并且降压活性大幅降低。
