Method for preparing 4-substituted chirality oxazolidinone compounds
A technology for oxazolidinones and compounds, applied in the field of preparation of chiral 4-substituted oxazolidinones, can solve problems such as potential safety hazards, and achieve the effects of reducing waste water discharge, reducing production costs, and reducing potential safety hazards
Active Publication Date: 2008-07-30
SUQIAN KEYLAB BIOCHEMICAL CO LTD
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Abstract
The invention relates to a preparation method of chiral 4-substituted oxazolidone, which belongs to the pharmaceutical chemistry technical field. Chiral amino acid ester or chiral amino acid ester salt is added into a solvent, supercarbonate is charged, chloro formate is titrated at the room temperature, and mixed for 5 to 8 hours at the room temperature after titration is completed, filtering is performed, and the solvent is recovered to obtain an intermediate compound a; the intermediate compound a is adopted in an anhydrous chloride solution for accelerating the catalyst of borohydride, reaction is performed for 4 to 10 hours at 0 to 40 DEG C, the solvent is recovered, a citric acid solution is added, extraction is performed by using ethyl acetate, an organic layer is combined, the solvent is recovered, and then an intermediate compound b is obtained; potassium carbonate is added into the intermediate compund b, heating, back flow and water diversion are performed for 2 to 4 hours, pump filtering is performed before cooling down, the filter liquor is cooled and recrystallized, pump filtering and drying are then performed to obtain a white crystalline solid 4-substituted chiral oxazolidone chemical compound. The invention provides the preparation method of a 4-substituted chiral oxazolidone chemical compound, the invention aims at the problem of significant safe hidden danger caused when phosgene is adopted for acidylation and cyclization in the prior art.
Application Domain
Asymmetric syntheses
Technology Topic
SolventBorohydride +20
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