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One of Hottest for Salicylic Acid - 8-Bromo-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3 – JIN DUN

One of Hottest for Salicylic Acid - 8-Bromo-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3 – JIN DUN

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One of Hottest for Salicylic Acid - 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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One of Hottest for Salicylic Acid - 8-Bromo-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3 – JIN DUN detail pictures


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The corporation upholds the philosophy of "Be No.1 in high quality, be rooted on credit rating and trustworthiness for growth", will continue to serve outdated and new consumers from home and overseas whole-heatedly for One of Hottest for Salicylic Acid - 8-Bromo-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3 – JIN DUN , The product will supply to all over the world, such as: Poland, luzern, Portugal, To keep the leading position in our industry, we never stop challenging the limitation in all aspects to create the ideal products. In his way, We can enrich our life style and promote a better living environment for the global community.
  • We are old friends, the company's product quality has been always very good and this time the price is also very cheap.
    5 Stars By Marina from Singapore - 2017.08.21 14:13
    It can be said that this is a best producer we encountered in China in this industry, we feel lucky to work with so excellent manufacturer.
    5 Stars By Madeline from Singapore - 2018.03.03 13:09
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