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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...
Bis(thien-2yl)methane is regioselectively lithiated at the inter-ring methylene carbon using dimsyl anion in THF at 0°C; quenching with appropriate electrophile furnishes meso-elaborated derivatives, exclusively with synthetic advantage.
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