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Merck
  • Highly versatile solid phase synthesis of biofunctional 4-aryl-3,4-dihydropyrimidines using resin-bound isothiourea building blocks and multidirectional resin cleavage.

Highly versatile solid phase synthesis of biofunctional 4-aryl-3,4-dihydropyrimidines using resin-bound isothiourea building blocks and multidirectional resin cleavage.

Bioorganic & medicinal chemistry letters (2000-01-15)
C O Kappe
RESUMEN

A series of pharmacologically active, functionalized 4-aryl-3,4-dihydropyrimidine-5-carboxylates (DHPMs) are prepared by a versatile novel solid phase approach. In the key step, a polymer-bound thiouronium salt is condensed with unsaturated 1-ketoesters. The resulting polymer bound 1,4-dihydropyrimidines are cleaved from the resin employing multidirectional resin cleavage strategies.

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Sigma-Aldrich
4-(Benzyloxy)benzyl chloride, 97%