An efficient solid phase synthetic route to 1, 3-disubstituted 2, 4 (1H, 3H)-quinazolinediones suitable for combinatorial synthesis

AL Smith, CG Thomson, PD Leeson

Index: Smith, Adrian L.; Thomson, Christopher G.; Leeson, Paul D. Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 13 p. 1483 - 1486

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Citation Number: 69

Abstract

Novel, efficient solid phase chemistry has been developed for the synthesis of 1, 3- disubstituted quinazolinediones. Anthranilic acids are linked to a chloroformate resin through the nitrogen, amines are coupled to the free carboxylic acid, and thermal cyclization leads to heterocycle formation and concommitant resin release resulting in traceless linkage.