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US 9,676,735 B2Granted
Process for the preparation of efavirenz and devices suitable therefore
AssigneeMax-Planck-Gesellschaft zur Forderung der Wissenschaften e.V.
InventorsCamille A. Correia, Kerry Gilmore, David Tyler McQuade, Peter H. Seeberger
Life of this patent
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Abstract
The invention relates to a process for the preparation of Efavirenz via an efficient transition metal catalyzed cyclization, to a device suitable to perform such process as well as to novel intermediates.
Claims19
A process for the preparation of 6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-1H-3,1-benzoxazin-2-one comprising reacting 4-cyclopropyl-2-(2,5-dichloro-phenyl)-1,1,1-trifluoro-but-3-yn-2-ol with at least one cyanate in the presence of at least one transition metal compound;
- wherein the at least one cyanate is selected from the group consisting of alkali cyanates and alkaline earth cyanates;
- and
- wherein the at least one transition metal compound is selected from the group consisting of copper, nickel, palladium, rhodium and platinum compounds.
Dependencies are inferred from the claim text.