Synthesis and Contractile Activity of Substituted 1,2,3,4-TetrahydroisoquinolinesReportar como inadecuado




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1

Department of Organic Chemistry, University of Plovdiv, 24 Tzar Assen Street, 4000 Plovdiv, Bulgaria

2

Department of Biophysics, Medical University, 15A Vasil Aprilov Street, 4000 Plovdiv, Bulgaria





*

Authors to whom correspondence should be addressed.



Abstract 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.

Keywords: Grignard reagent; tetrahydroisoquinolines; contractile activity Grignard reagent; tetrahydroisoquinolines; contractile activity





Autor: Iliyan Ivanov 1,* , Stoyanka Nikolova 1, Dimo Aladjov 1, Iliyana Stefanova 2 and Plamen Zagorchev 2,*

Fuente: http://mdpi.com/



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