Rodney L. Parsons

TL;DR: In this article, a highly enantioselective and practical synthesis of the HIV-1 reverse transcriptase inhibitor efavirenz (1) is described, which proceeds in 62% overall yield in seven steps from 4-chloroaniline (6) in excellent chemical and optical purity.

TL;DR: This reaction provides an efficient route to the second generation NNRTI drug candidate DPC 963 by using enantiopure amino alcohol as a chiral moderator for the addition of lithium cyclopropylacetylide to an unprotected N-acylketimine.

TL;DR: The present paper relates to benzoxazinones of formula I, or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, methods of using same for treating viral infection or as an assay standard or reagent, and intermediates and processes for making the same as discussed by the authors.

TL;DR: Two series of efavirenz analogues have been developed: one in which the cyclopropane ring has been replaced by small heterocycles and another inWhich the entire acetylenic side chain has been replacement by alkyloxy groups.

TL;DR: The practical and highly diastereoselective syntheses of CF(3)-substituted dihydroquinazolinones via 1,4-additions of nucleophiles to chiral auxiliary substituted 2(3H)-quinazolones is described.