Begum Sabira, Ali Syed Nawazish, Hassan Syed Imran, Siddiqui Bina S
H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan.
Molecules. 2008 Aug 6;13(8):1584-98. doi: 10.3390/molecules1301584.
A simple, rapid, solvent-free, room temperature one pot synthesis of benzene ring acylated and demethylated analogues of harmine using acyl halides/acid anhydrides and AlCl(3) has been developed. Eight different acyl halides/acid anhydrides were used in the synthesis. The resulting mixture of products was separated by column chromatography to afford 10- and 12-monoacyl analogues, along with 10,12-diacyl-11-hydroxy products. In five cases the corresponding 10-acyl-11-hydroxy analogues were also obtained. Yields from the eight syntheses (29 products in total) were in the 6-34% range and all compounds were fully characterized.
已开发出一种简单、快速、无溶剂、室温一锅法合成方法，使用酰卤/酸酐和氯化铝（AlCl₃）合成哈尔明的苯环酰化和去甲基化类似物。合成过程中使用了八种不同的酰卤/酸酐。通过柱色谱法分离所得产物混合物，得到10-和12-单酰基类似物以及10,12-二酰基-11-羟基产物。在五种情况下还获得了相应的10-酰基-11-羟基类似物。这八种合成方法（总共29种产物）的产率在6-34%范围内，并且所有化合物均得到了充分表征。
