An efficient two-step procedure is described to convert the Biginelli 3,4-dihydropyrimidin-2(1H)-one to various multifunctionalized pyrimidines via the Kappe dehydrogenation and a new mild PyBroP-mediated coupling with C, N, O, and S nucleophiles, which provides a readily accessible multifunctionalized pyrimidine template for diversity-oriented synthesis.

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Affinity. -The structure-activity relationships of several novel synthesized compounds such as (III) and (V) are discussed in detail (no yields given). (IIIc) and (V) possess potent 5-HT-T affinity and moderately potent 5-HT1A affinity. -(GILBERT*, A. M.; COLEMAN, T.; KODAH, J.; MEWSHAW, R. E.; SCERNI, R.; SCHECHTER, L. E.; SMITH, D. L.; ANDREE, T. H.; Bioorg. Med.