Bifunctional Cinchona Alkaloid Thiourea Catalyzed Highly Efficient, Enantioselective Aza‐Henry Reaction of Cyclic Trifluoromethyl Ketimines: Synthesis of Anti‐HIV Drug DPC 083

Abstract

Highly efficient: The title reaction provides biologically interesting chiral trifluoromethyl dihydroquinazolinone frameworks in high yields (up to 97 %) and with high enantioselectivities (up to 98 % ee), using as low as 1 mol % of catalyst (see scheme). Moreover, anti-HIV drug candidate DPC 083 was efficiently synthesized using the highly enantioselective aza-Henry reaction as a key step. Detailed facts of importance to specialist readers are published as ”Supporting Information”. Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.