Efavirenz is an essential medicine for the treatment of HIV, which is still inaccessible to millions of people worldwide. A novel, semi-continuous process provides rac-Efavirenz with an overall yield of 45%. This streamlined proof-of-principle synthesis relies on the efficient copper-catalyzed formation of an aryl isocyanate and a subsequent intramolecular cyclization to install the carbamate core of Efavirenz in one step. The three-step method represents the shortest synthesis of this life-saving drug to date.

A palladium-catalyzed coupling of N-heterocycles with simple alcohols was achieved. The reaction is initiated by peroxide and does not require the use of stoichiometric acid for activation of the heterocycle.

The activation of benzylic C À H bonds and subsequent coupling with terminal alkynes in the presence of 2,3-dichloro-5,6-dicyanoquinone (DDQ) and a catalytic amount of copper(I) triflate is presented. Good to moderate yields of disubstituted alkynes are obtained for this cross-dehydrogenative coupling (CDC) reaction between a variety of aromatic alkynes and diphenylmethane derivatives.

An efficient Grignard-type arylation of aldehydes via aryl C À H activation was achieved under mild conditions catalyzed by rhodium. The reaction provides an easy access to a wide variety of benzyl alcohols and can tolerate various functional groups as well as air and water.

An efficient rhodium(III)-catalyzed C-H activation and subsequent conjugate addition was achieved under mild conditions. The reaction utilized inert arenes to replace stoichiometric organometallic reagents and can tolerate various functional groups as well as air and water.