Method for synthesizing SGLT2 inhibitor drugs

A synthesis method and drug technology, applied in the field of preparation of small molecule chemical drugs, can solve the problems of difficult operation, cumbersome, high equipment requirements, etc., and achieve the effect of shortening the reaction steps, simplifying the operation method, and simple process steps
CN104710486AInactive Publication Date: 2015-06-17ARROMAX PHARMATECH
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ARROMAX PHARMATECH
Publication Date
2015-06-17
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides a method for synthesizing SGLT2 inhibitor drugs. The method comprises the following steps: (a) reacting a compound (1) with n-butyllithium in an organic solvent for 0.5-2 hours, and then dripping an organic solvent dissolved with a compound (2) to react for 1.5-4 hours to obtain a compound (3); or, in a nitrogen atmosphere, reacting the compound (1) with isopropylmagnesium chloride and lithium chloride in the organic solvent for 0.5-1 hour, and then dripping the organic solvent dissolved with the compound (2) to react for 1.5-4 hours to obtain the compound (3); (b) in the organic solvent, carrying out a reduction reaction on the compound (3) to obtain a compound (4); (c) in the organic solvent, carrying out an acetylation reaction on the compound (4), pyridine and acetic anhydride to obtain a compound (5); and (d) carrying out a hydrolysis reaction on the compound (5) to obtain a compound (6), namely the SGLT2 inhibitor drugs. The method provided by the invention is simple in steps, low in cost, high in yield and is suitable for industrial production. The reaction route is as follows in the specification.
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Description

technical field

[0001] The present invention relates to the field of preparation of small molecular chemical medicines, and more particularly relates to a synthesis method of a net drug. Background technique

[0002] Sodium-dependent glucose cotransporters (SGLTs) are divided into SGLT1-6, among them, SGLT2 has high capacity and low affinity, responsible for 90% glucose reabsorption, while SGLT1 only completes 10% glucose reabsorption, therefore, inhibits the activity of SGLT2 , increase the excretion of glucose by the kidneys, and become a new target for the development of a new generation of antidiabetic drugs.

[0003] In recent years, the U.S. Food and Drug Administration (FDA) has successively approved the listing of three drugs of the same class, which are Dapagliflozin, Canagliflozin and Empagliflozin. Both are sodium-glucose cotransporter II inhibitors (SGLT2) for the treatment of type II diabetes.

[0004] Dapagliflozin, the chemical name is 2-chloro-5-(D-glucopyr...

Claims

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