取代的 1,2,3,4-四氢异喹啉的合成和收缩活性。
Synthesis and contractile activity of substituted 1,2,3,4-tetrahydroisoquinolines.
机构信息
Department of Organic Chemistry, University of Plovdiv, 24 Tzar Assen Street, 4000 Plovdiv, Bulgaria.
出版信息
Molecules. 2011 Aug 16;16(8):7019-42. doi: 10.3390/molecules16087019.
A series of different 1-monosubstituted and 1,1-disubstituted 1,2,3,4-tetrahydro-isoquinolines was synthesized in high yields from different ketoamides. We have developed a convenient method for the synthesis of disubstituted derivatives by interaction of ketoamides with organomagnesium compounds, followed by cyclization in the presence of catalytic amounts of p-toluenesulfonic acid (PTSA). A number of substituents at the C-1 in the isoquinoline skeleton were introduced varying either carboxylic acid or organomagnesium compound. Some of the obtained 1,1-dialkyl-1,2,3,4-tetrahydro-isoquinolines possess contractile activity against guinea pig's gastric smooth muscle preparations.
我们从不同的酮酰胺出发，高产率地合成了一系列不同的 1-单取代和 1,1-二取代的 1,2,3,4-四氢异喹啉。我们开发了一种方便的方法，通过酮酰胺与有机镁化合物的相互作用，随后在催化量的对甲苯磺酸（PTSA）存在下环化，来合成二取代衍生物。在异喹啉骨架的 C-1 上引入了许多取代基，取代基可以是羧酸或有机镁化合物。一些得到的 1,1-二烷基-1,2,3,4-四氢异喹啉对豚鼠胃平滑肌制剂具有收缩活性。
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