Synthetic method of empagliflozin

A synthetic method and compound technology, applied in drug combination, organic chemistry, metabolic diseases, etc., can solve the problems of low total yield, high cost, instability, etc.
CN110698467AActive Publication Date: 2020-01-17HUANGGANG LUBAN PHARM
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
HUANGGANG LUBAN PHARM
Publication Date
2020-01-17

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Abstract

The invention provides a brand-new synthesis process of empagliflozin. According to the process, a boric acid ester is used for halogen removal, and specific reaction conditions are combined, so thatempagliflozin can be prepared with high yield and simplicity and convenience in operation. The synthesis method of empagliflozin has the advantages of mild reaction conditions, high total yield, few side reactions and convenience in operation, thereby being beneficial to industrial production and cost control.
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Description

technical field

[0001] The invention belongs to the field of medicine and fine chemical industry. Specifically, the present invention relates to a new synthesis method of Empagliflozin and a new intermediate for the synthesis of Empagliflozin. Background technique

[0002] Empagliflozin is a selective oral SGLT-2 inhibitor developed by Boehringer Ingelheim, and is a new type of oral hypoglycemic drug. It was first launched in Europe in May 2014, in the United States and Japan in August and December 2014, and in China in September 2017. Empagliflozin can selectively inhibit the reabsorption of filtered glucose by the proximal tubules of the glomerulus, excrete excess glucose from the urine, and directly lower blood sugar. It is used for the treatment of type II diabetes. And has good safety and tolerance.

[0003] The scientific name of Englie purification is: (1S)-1,5-anhydro-1-C-(4-chloro-3-((4-((((3S)-tetrahydro-3-furyl)oxy ) phenyl) methyl) phenyl) -D-glucitol. Empagl...

Claims

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