Lushi Tan

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: Kilogram-scale synthesis of the HIV reverse transcriptase inhibitor efavirenz was achieved by means of a highly enantioselective alkynylation of prochiral ketones 1 with alkynyllithium or alkynymagnesium reagents in the presence of chiral zinc aminoalkoxides as mediators.

TL;DR: An efficient rhodium-catalyzed method for direct C-H functionalization at the C7 position of a wide range of indoles has been developed, with good to excellent yields of alkenylation products.

TL;DR: Dynamic kinetic resolution (deracemization) of various alpha-alkyl-substituted beta-ketoamides 1 via asymmetric transfer hydrogenation proceeded efficiently to give the corresponding syn-beta-hydroxy amides 3 in high diastereo- and enantioselectivities.

TL;DR: A practical preparation of an alpha(v)beta(3) antagonist is reported, which consists of three key components, a tetrahydronaphthyridine moiety, a beta-alanine moieties, and a central imidazolidone moiety.