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33.4.18.1.1.1.4 Variation 4: Solid-Phase Hantzsch Synthesis

DOI: 10.1055/sos-SD-033-00648

Quirion, J.-C.; Leclerc, E.; Jubault, P.Science of Synthesis, (200733604.

Despite the convenience of the one-pot, three-component reaction, the great potential of Hantzsch 1,4-dihydropyridines as therapeutic agents had instigated the development of combinatorial libraries. The prerequisite for such libraries is the elaboration of solid-phase synthesis techniques.[‌18‌,‌19‌] One achievement in this area has been the development of a procedure using Rink resin, and a library of 300 1,4-dihydropyridines has been created.[‌20‌] The free-amine resin reacts with several β-oxo esters to form a pool of immobilized enamines 6. The condensation with aldehydes and other 1,3-dicarbonyl compounds allows the synthesis of 1,4-dihydropyridines 7 after acid-promoted cleavage of the resin (Scheme 6).

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