Method for preparing remimazolam
A technology of remimazolam and an intermediate, which is applied in the field of preparation of labor pain anesthetic drug remazolam, can solve problems such as waste, and achieve the effects of improving quality, optimizing preparation process and simple operation.
Active Publication Date: 2021-11-30
SHANGHAI ZAIQI BIO TECH
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Abstract
The invention discloses a preparation method of remimazolam, and belongs to the technical field of medical intermediates. The preparation method comprises the following steps: carrying out condensation on 2-(2-amino-5-bromo-benzoyl) pyridine (1) and BOC-glycine to obtain an intermediate (2); removing Boc protection from the intermediate (2), and performing ring closing to obtain an intermediate (3); performing sulfonylation and substitution reaction on the intermediate (3) to obtain an intermediate (4); oxidizing and cyclizing the intermediate (4) to obtain an intermediate (5); and reacting the intermediate (5) with methyl acrylate, and carrying out chiral resolution to obtain remimazolam (6). The production of an impurity II is avoided, and the quality of the product is improved; and after the resolution, the configuration is not required, alkali can be continuously added for racemization, and the resolution is performed again, so that the process reproducibility is good, and the reaction scale can be smoothly enlarged to a kilogram-level reaction scale.
Application Domain
Organic chemistry methodsBulk chemical production
Technology Topic
Chiral resolutionPyridyne +9
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