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Omarigliptin intermediate preparation method

A technology for intermediates and compounds, applied in the field of preparing aulogliptin intermediates, can solve the problems of expensive catalysts, high process production costs, serious environmental pollution, etc., achieves improved yield and atom economy, and is suitable for large-scale industrialization Production, environmentally friendly effects

Active Publication Date: 2017-05-31
SUZHOU LEAD BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The technical problem to be solved by the present invention is that the production cost of the process for preparing the alogliptin intermediate in the prior art is high, the catalyst for the reaction is expensive, the environment is polluted seriously, and the reaction produces by-products. High efficiency, easy to prepare, and more environmentally friendly method for the preparation of alogliptin intermediates

Method used

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preparation example Construction

[0034] The synthetic route of the method for preparing augliptin intermediate described in embodiment 1-6 is:

[0035]

Embodiment 1

[0037] The method for preparing the alogliptin intermediate in this embodiment is specifically:

[0038] Take 1g of the compound I and 1.25g of glucose in a 100mL three-necked flask, and then add 50mL of PBS buffer solution with a pH value of 6.5 and a concentration of 0.05mol / L; put the three-necked flask into the reaction pot, set the speed 850rpm, temperature 30℃, then add 5mg NADP respectively + , 5mg NAD + , 20mg glucose dehydrogenase (purchased from Suzhou Pivot Biotechnology Co., Ltd., product number is YH1901, here only provides one of the products of the model to set forth the effect of the present invention, between commercially available products of each model for the realization of the present invention There is no difference in the purpose of the invention, the same below, and will not be repeated later), and 100mg ketoreductase powder (purchased from Suzhou Pivot Biotechnology Co., Ltd.), to obtain a mixed solution, and make the mixed solution at a temperature o...

Embodiment 2

[0044] The method for preparing the alogliptin intermediate in this embodiment is specifically:

[0045] Take 5g of the compound I and 6.25g of glucose in a 100mL three-necked flask, add 50mL of PBS buffer solution with a pH value of 6.5 and a concentration of 0.05mol / L; put the three-necked flask into a reaction pot, set the speed at 850rpm, and the temperature at 30°C , and then add 5mg NADP respectively + , 100mg glucose dehydrogenase, and 200mg ketoreductase powder (purchased from Suzhou Pivot Biotechnology Co., Ltd., product number is YH2033, only one of the models is given here to illustrate the effect of the present invention, commercially available models There is no difference between the products for realizing the purpose of the present invention, the same below, no more redundant description hereinafter), to obtain a mixed solution, to make the mixed solution react at a temperature of 30°C, and meanwhile, use 2mol The NaOH solution of / L maintains the pH value of t...

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Abstract

The invention provides an omarigliptin intermediate preparation method. The omarigliptin intermediate preparation method comprises the step of mixing a compound I with a catalyzing enzyme, and reacting to obtain an omarigliptin intermediate. The omarigliptin intermediate preparation method has the beneficial effects that the cost of raw materials is reduced; the problem in the prior art that isomer byproducts are generated during preparation of the omarigliptin intermediate and cannot be utilized is effectively solved; the yield and atom economy are increased; and the omarigliptin intermediate preparation method is simple in operation, mild in conditions, environment-friendly and suitable for industrial production.

Description

technical field [0001] The invention relates to a method for preparing an alogliptin intermediate, belonging to the technical fields of biopharmaceuticals and biochemical industries. Background technique [0002] Diabetes is a group of metabolic diseases characterized by high blood sugar, which seriously endangers people's health. my country is a big country with diabetes. According to the latest research results, among the adult samples aged 18 and above in my country, the estimated prevalence of diabetes is 11.6%, or 113.9 million people; among them, the prevalence of prediabetes (IGT) is 50.1%. , that is, half of the people are the reserve army of diabetes. This set of figures profoundly reveals the grim situation of diabetes in my country. [0003] Alogliptin (MK-3102) is an ultra-long-acting dipeptidyl peptidase-4 (DPP-4) inhibitor oral hypoglycemic drug developed by Merck & Co. of the United States. Alogliptin has the advantages of less toxic and side effects, high d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12P13/00
CPCC12P13/001
Inventor 谢新开黄晓飞张金鑫张瑞杰
Owner SUZHOU LEAD BIOTECH CO LTD
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