General Scope of 1, 4-Diastereoselective Additions to a 2 (3 H)-Quinazolinone: Practical Preparation of HIV Therapeutics

NA Magnus, PN Confalone, L Storace…

Index: Magnus, Nicholas A.; Confalone, Pat N.; Storace, Louis; Patel, Mona; Wood, Christopher C.; Davis, Wayne P.; Parsons Jr., Rodney L. Journal of Organic Chemistry, 2003 , vol. 68, # 3 p. 754 - 761

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Citation Number: 35

Abstract

The practical and highly diastereoselective syntheses of CF3-substituted dihydroquinazolinones via 1, 4-additions of nucleophiles to chiral auxiliary substituted 2 (3 H)-quinazolinones is described. This methodology is applied to the syntheses of the NNRTIs (nonnucleoside reverse transcriptase inhibitors) DPC 961 (1) and DPC 083 (2), which are useful for the treatment of HIV (human immunodeficiency virus). The synthesis of DPC 961 ...