Method for synthesizing intermediate benzene sulfonamide of type 2 diabetes mellitus drug glimepiride

A technology for isobenzenesulfonamide and diabetes drugs, which is applied in the field of compound preparation, can solve the problems of complex process steps and inconvenient operation, and achieve the effect of simple process and high product yield
CN103288703AInactive Publication Date: 2013-09-11姜树林
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
姜树林
Publication Date
2013-09-11
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a method for synthesizing the intermediate benzene sulfonamide of type 2 diabetes mellitus drug glimepiride. The method comprises the following steps of: reacting phenylethylamine with 3-ethyl-4-methylpyrrolinone in a solvent under the conditions that a certain temperature is controlled and phosgene is introduced, and after the reaction, performing corresponding treatment to obtain N-[2-(3-ethyl-4-methyl-2-oxo-3-pyrroline-1-formylamino)ethyl] benzene (3), and reacting the N-[2-(3-ethyl-4-methyl-2-oxo-3-pyrroline-1-formylamino)ethyl] benzene (3) with chlorosulfonic acid to obtain a sulfonated product; reacting the sulfonated product with ammonia water to obtain the crude product of benzene sulfonamide, and then performing solvent refining to obtain the finished product. A reaction formula involved is as shown in the specification. The method provided by the invention is simple in process, easy to operate and high in product yield.
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Description

[0001] technical field

[0002] The invention relates to a method for synthesizing benzenesulfonamide, an intermediate of glimepiride, a drug for type II diabetes, and belongs to the field of compound preparation. Background technique

[0003] Glimepiride is a third-generation sulfonylurea oral hypoglycemic drug. The main mechanism of its hypoglycemic effect is to stimulate the secretion of insulin by pancreatic β cells and partially increase the sensitivity of surrounding tissues to insulin. This product binds and dissociates faster than glibenclamide with the insulin receptor, and causes less severe hypoglycemia. After oral administration, glimepiride is 100% absorbed in the gastrointestinal tract. The plasma concentration reaches the peak (Cmax) within 2-3 hours, and the protein binding rate is greater than 99.5%. Glimepiride is completely metabolized through oxidative biotransformation, the main metabolites are cyclohexyl hydroxymethyl derivatives (M1) and carboxylated...

Claims

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