Good quality 99% 2-Cyanobenzyl Bromide; Alpha-Bromo-O-Toluonitrile CAS: 22115-41-9

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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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Good quality China 2-Cyanobenzyl Bromide Powder and Alpha-Bromo-O-Toluonitrile, We strongly believe that technology and service is our base today and quality will create our reliable walls of future. Only we’ve better and better quality , could we achieve our customers and ourselves, too. Welcome customers all over the word to contact us for getting further business and reliable relationships. We have been always here working for your demands whenever you will need.