OEM/ODM Supplier Adhensive For Drilling Fluid 80a-51 - 8-Bromo-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3 – JIN DUN

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Sticking to the perception of "Creating products of top of the range and earning mates with people today from all over the world", we constantly put the desire of consumers in the first place for Superhydrophobic, Chlorination Process In Water Treatment, Water Softener And Filtration System, We believe that in good quality more than quantity. Before export of the hair there is strict top quality control check during treatment as per international good quality standards.

OEM/ODM Supplier Adhensive For Drilling Fluid 80a-51 - 8-Bromo-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3 – JIN DUN Detail:

Use: Intermediate for Linagliptin.

Use：Intermediate for Linagliptin
Executive standard： enterprise standard
Assay：98-102%

Exterior：White to light yellow powder
Package: 25kg/drum

To analyze the existing linagliptin and its key intermediate 8-bromo-7-(2-butynyl)-3,7-dihydro-3-methyl-1-[(4-methyl -2-quinazolinyl)methyl)-1H-purine-2,6-dione (11) synthesis method, find a synthetic route suitable for industrial production. Method: summarize the different synthetic routes. Results and conclusions: Route 2.2 has a relatively simple process and lower cost, which is more suitable for industrial production.

8-bromo-3,7-dihydro-3-methyl-1H-purine-2,6-dione is a key intermediate in the synthesis of the hypoglycemic drug linagliptin. The synthesis of 1 uses methyl urea and cyanoacetic acid as starting materials, and undergoes six-step reactions of condensation, cyclization, nitrosation, reduction, cyclization, and bromine with a total yield of 46.3%. The structures of all intermediates were confirmed by 1HNMR.

The present invention relates to a simple preparation method of high-purity linagliptin. Quinazoline, the key intermediate for the one-pot preparation of linagliptin 8 bromo 7 (2 butyne 1 base) 3,7 dihydro 3 methyl 1 [(4 methyl 2 quinazolinyl) methyl] 1H Purine 2,6 dione, the intermediate is separated by filtration, and then reacted with (R)3 aminopiperidine dihydrochloride to obtain a solution containing linagliptin. After the solution containing linagliptin is processed again, Deliraliptin pure product. The preparation of the key intermediate of the present invention adopts a one-pot method, which is convenient to operate and improves the yield. After the key intermediate is separated, it is reacted with (R)3 aminopiperidine dihydrochloride, thereby Obtaining high-purity linagliptin also meets the production and declaration requirements of pharmaceutical companies to the greatest extent.

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