The present invention relates generally to novel methods for the preparation of cyclopropylacetylene which is an essential reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-ben zoxazin-2-one; a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor with superior anti-retroviral activity. In the process, for example, cyclopropane carboxaldehyde is alkylated to form 1,1,1-trichloro-2-cyclopropyl-ethanol; which in turn undergoes elimination to form 1,1-dichloro-2-cyclopropyl-ethene; which in turn undergoes elimination to form cyclopropyl acetylene.

A invenção atual relaciona-se geralmente aos métodos da novela para a preparação do cyclopropylacetylene de que é um reagent essencial na síntese asymmetric (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-ben zoxazin-2-one; um inibidor reverso humano útil do transcriptase do vírus do immunodeficiency (HIV) com atividade anti-retroviral superior. No processo, para o exemplo, o carboxaldehyde do cyclopropane alkylated para dar forma a 1,1,1-trichloro-2-cyclopropyl-ethanol; qual se submete por sua vez ao elimination para dar forma a 1,1-dichloro-2-cyclopropyl-ethene; qual se submete por sua vez ao elimination para dar forma ao acetileno do cyclopropyl.