A kind of preparation method of voglibose impurity I hydrochloride

A technology of voglibose and hydrochloride, which is applied in the field of medicine, can solve the problems of impurity I not yet prepared, and achieve the effects of improving drug safety, simple process flow, and improving quality standards

Active Publication Date: 2020-11-03
无锡富泽药业有限公司
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  • Abstract
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  • Claims
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Problems solved by technology

[0007] The above three impurities are mixed and controlled for system suitability experiment and impurity control. Impurity I and impurity II are isomers. At present, there is no report on the preparation of impurity I

Method used

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  • A kind of preparation method of voglibose impurity I hydrochloride
  • A kind of preparation method of voglibose impurity I hydrochloride
  • A kind of preparation method of voglibose impurity I hydrochloride

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Embodiment Construction

[0029] The present invention will be described in detail below with reference to the embodiments shown in the drawings. However, it should be noted that these embodiments do not limit the present invention, and those of ordinary skill in the art make functional, method, or structural improvements based on these embodiments. Equivalent changes or substitutions fall within the protection scope of the present invention.

[0030] The invention discloses a preparation method of voglibose impurity I hydrochloride, and the overall reaction process formula is:

[0031]

[0032] Specifically include the following steps:

[0033] Step 1: (S)-(Ethylene oxide methyl) carbamic acid tert-butyl ester and tetrabenzyl tetrabenzyl mycosylamine undergo epoxide amination to obtain the compound of formula III, namely tert-butyl ((2S)-3- Hydroxy-2-(((2S,3R,4S,5S)-2,3,4-tris(benzyloxy)-5-((benzyloxy)methyl)-5-hydroxycyclohexyl)amino)propane 基)tert-butyl carbamate;

[0034] The specific method is as follows...

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Abstract

The present invention provides a kind of preparation method of voglibose impurity I hydrochloride, comprising the steps of: (S)-(oxirane methyl) carbamate tert-butyl ester and tetrabenzyl Jinggang mycosamine Amination of epoxide to obtain the compound of formula III; the hydroxyl group of the compound of formula III is protected by benzyl group to obtain the compound of formula IV; the amino protecting group of the compound of formula IV is deprotected to obtain the compound of formula V; 5S)-5-hydroxyl-2,3,4-tris(benzyloxy)-5-[(benzyloxy)methyl]-cyclohexanone undergoes a condensation reduction reaction to obtain a compound of formula VI. The preparation method of voglibose impurity I hydrochloride provided by the present invention has a simple process flow and fills up the gap in the current technology for preparing voglibose impurity I. The prepared voglibose impurity I hydrochloride The salt can be used for qualitative and quantitative research on impurities in the production of voglibose, which can improve the quality standard of voglibose, thereby improving the drug safety of voglibose.

Description

Technical field [0001] The invention relates to the technical field of medicine, in particular to a method for preparing voglibose impurity I hydrochloride. Background technique [0002] Voglibose, chemical name (+)-1L-[1(hydroxy), 2,4,5 / 3]-5-[2-hydroxy-1-(hydroxymethyl)ethyl]amino-1 -(Hydroxymethyl)-1,2,3,4-cyclohexanetetraol, CAS: 83480-29-9, has the chemical structure shown in the following formula: [0003] [0004] Voglibose was first developed by Japan’s Takeda Company. It was first marketed in Japan under the trade name "Basen" in 1994, Korea in 1998, and China in 1999 for the treatment of diabetic postprandial blood glucose increase. In 2009, Voglibose was included in the "National Basic Medical Insurance, Industrial and Commercial Insurance and Maternity Insurance Drug Catalog." At present, voglibose is widely used in the prevention, treatment and combination medication of type I and type II diabetes. Compared with sulfonylureas, voglibose does not stimulate insulin sec...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C213/00C07C215/42
CPCC07C213/00C07C269/06C07C2601/14C07C271/20C07C217/52C07C215/42Y02P20/55
Inventor 胡新祥吴鹏程张允果谢卫锋
Owner 无锡富泽药业有限公司
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