Synthesis and Contractile Activity of Substituted 1,2,3,4-Tetrahydroisoquinolines

Molecules

关键词: Grignard reagent;    tetrahydroisoquinolines;    contractile activity;   

DOI  :  10.3390/molecules16087019

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown