1219204-23-5Relevant articles and documents
Preparation method for bicyclic pyrrolidine intermediate of telaprevir
-
Paragraph 0025; 0045, (2017/01/17)
The invention discloses a preparation method for a bicyclic pyrrolidine intermediate of telaprevir. The intermediate is (1S,3alphaR,6alphaS)-octahydrocyclopenta[c]pyrrole-1-carboxylic acid-ethyl ester hydrochloride. The preparation method comprises the following steps: (1) with 3-azabicyclo[3.3.0]octane hydrochloride as a raw material, carrying out Boc2O protection under the action of inorganic base so as to obtain an intermediate 1; (2) dissolving the intermediate 1 in an organic solvent, adding chiral organic ligand, carrying out a reaction with lithium alkyl at -70 DEG C for 2 h under the protection of nitrogen and introducing dry carbon dioxide so as to obtain an intermediate 2; and (3) adding the intermediate 2 into a saturated hydrogen chloride ethanol solution and carrying out a heating reflux reaction for 3 h so as to obtain the target compound. The preparation method provided by the invention has the advantages of short synthesis route, low cost, high product yield and optical purity and easiness in realization of large-scale production.
BIOCATALYTIC PROCESSES FOR THE PREPARATION OF SUBSTANTIALLY STEREOMERICALLY PURE FUSED BICYCLIC PROLINE COMPOUNDS
-
Page/Page column 96, (2010/04/03)
The present disclosure provides substantially stereomerically pure fused bicyclic proline compounds of structural Formulae II to VII as described herein, and to biocatalytic processes for their preparation, and to the enzymes used in those processes.
