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Molecules 2011, 16(8), 7019-7042; doi:10.3390/molecules16087019
Article

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

1,* , 1, 1, 2 and 2,*
Received: 22 July 2011; in revised form: 10 August 2011 / Accepted: 11 August 2011 / Published: 16 August 2011
(This article belongs to the Special Issue Heterocycles)
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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
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Ivanov, I.; Nikolova, S.; Aladjov, D.; Stefanova, I.; Zagorchev, P. Synthesis and Contractile Activity of Substituted 1,2,3,4-Tetrahydroisoquinolines. Molecules 2011, 16, 7019-7042.

AMA Style

Ivanov I, Nikolova S, Aladjov D, Stefanova I, Zagorchev P. Synthesis and Contractile Activity of Substituted 1,2,3,4-Tetrahydroisoquinolines. Molecules. 2011; 16(8):7019-7042.

Chicago/Turabian Style

Ivanov, Iliyan; Nikolova, Stoyanka; Aladjov, Dimo; Stefanova, Iliyana; Zagorchev, Plamen. 2011. "Synthesis and Contractile Activity of Substituted 1,2,3,4-Tetrahydroisoquinolines." Molecules 16, no. 8: 7019-7042.



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