| 摘要 |
Provided is a synthesis process for a chiral cyclopropyl ethynyl tertiary alcohol compound. With regard to the process of the present invention, a chiral amino alcohol or a chiral amino diol is reacted as a ligand in the presence of an alkaline reagent and a salt to obtain an optically active propynyl alcohol compound. In particular, the process of the present invention comprises the following steps: (1) reacting cyclopropyl acetylene with a chiral inducing agent, a chiral auxiliary reagent and zinc halide in an organic solvent in the presence of an alkaline reagent and a sulfonate or a sulphinate to obtain a first reaction mixture; (2) reacting the resultant first reaction mixture with 5-chloro-2-aminotrifluorobenzophenone to form (S)-2-amino-5-chloro-α-cyclopropyl acetylene-α-trifluoromethylbenzyl alcohol. The process of the present invention avoids the use of an organic zinc reagent and a Grignard reagent, and has the advantages of safe production, an environmentally friendly route, low production costs, a high resultant product yield, a high chiral ee value and the like, and is suitable for industrial production. |
