Method of preparing esopiclone intermediate 6-(5-chloro-2-pyridyl)-5-hydro-7-oxy-6,7-dihydro-5H-pyrrolo[3,4-b] pyrazine

Abstract

The invention discloses a making method of 6-(5-chlorine-2-pyridinyl)-5-hydroxide-7-oxy-6,7-dihydrogen-5H-pyrrole [3,4-b] as intermediate of dextro-mated clone,which comprises the following steps: dissolving 6-(5-chlorine-2-pyridinyl)-5, 7-dioxy6, 7-dihydrogen-5H-pyrrole [3,4-b] pyrazine in the organic solvent or organic solvent with water; adding acylorxy radical sodium / potassium borohydride in the reacting liquid; or adding organic acid, sodium borohydride or potassium borohydride sequently; washing into water after reacting; stewing; filtering; obtaining the product.

Description

technical field The invention relates to a preparation method of a chemical drug intermediate, specifically, an intermediate 6-(5-chloro-2-pyridyl)-5-hydroxyl-7-oxo- Process for the preparation of 6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine. Background technique Drugs clinically used for the treatment of insomnia mainly include barbiturates (first generation), benzodiazepines (second generation), non-benzodiazepines (third generation) and traditional Chinese medicines. The market of first-generation and second-generation anti-insomnia drugs shows a clear downward trend due to the large side effects and the tendency to generate dependence and tolerance. The third-generation non-benzodiazepine hypnotics can selectively act on BZ1 receptors, and the residual effects produced are relatively small, and the phenomenon of "sleeping" is rarely produced in the next morning, and does not affect the mental activity and alertness of movements in the next morning. Degree, and the dose is sma...

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Problems solved by technology

The above-mentioned methods all can only obtain the reduction product of medium yield, and dissolving metal borohydride with aqueous dioxane is dangerous to a certain extent.

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