| abstract |
"PROCESS FOR THE SYNTHESIS OF CYCLOPROPYLACETYLENE AND COMPOUND" The present invention relates, in general, to innovative methods for the synthesis of cyclopropylacetylene, which is an essential reagent in the asymmetric synthesis of (S) -6-chloro-4-cyclopropylethylyl -4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazine-2-one; a useful inhibitor of human immunodeficiency virus (HIV) reverse transcriptase. In the process, cyclopropane carboxaldehyde is condensed with malonic acid in order to form 3-cyclopropylacrylic acid; 3-cyclopropylacrylic acid is halogenated to form (E, Z) -1-halo-2-cyclopropylethylene; and (E, Z) -1-halo-2-cyclopropylethylene is dehydrohalogenated in order to form cyclopropyl acetylene. This improvement provides high conversion of easily available and low-cost starting materials into cyclopropylacetylene, high global production and can be carried out on an industrial scale. |