Regioselective addition reactions at C-2 of 3,4-dihydropyrimidinones. Synthesis and evaluation of multifunctionalized tetrahydropyrimidines |
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| Authors: | Kamaljit Singh Divya Arora |
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| Affiliation: | a Organic Synthesis Laboratory, Department of Applied Chemical Sciences & Technology, Guru Nanak Dev University, Amritsar, Punjab 143 005, India
b Rega Institute for Medical Research, Katholieke Universiteit Leuven, 10 Minderbroedersstraat, B-3000 Leuven, Belgium |
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| Abstract: | Multifunctionalized tetrahydropyrimidines derivatives have been synthesized from Biginelli 3,4-dihydropyrimidin-2-(1H)-thiones (DHPMs) efficiently. The transformation includes desulfurization of DHPMs with Raney-Ni and subsequent regioselective C-2 functionalization using a variety of C-nucleophiles with simultaneous activation with ethyl chloroformate. Functionalized pyrimidine derivatives containing bulky substituents at C-2 of the pyrimidine ring are cytostatic. |
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| Keywords: | Biginelli compounds Carbon nucleophiles Pyrimidines Regioselectivity Desulfurization |
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