Electric Literature of 94741-69-2, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.94741-69-2, name is 4-Amino-2-chloro-5-pyrimidinecarbonitrile, molecular formula is C5H3ClN4, molecular weight is 154.56, as common compound, the synthetic route is as follows.
Step 5A: (2R)-4-(4-arnino-5-cvanopyrirnidin-2-yl)-N-[2-(l-benzylpiperidin-4- yl)ethyll-2-methylpiperazine-l -carboxamide (0311) To a solution of (2R)-N-[2-(l-benzylpiperidin-4-yl)ethyl]-2- methy lpiperazine- 1 -carboxamide 4a (0.20 g, 0.58 mmol, 1.0 eq) and 4-amino-2- chloropyrimidine-5-carbonitrile (0.90 g, 0.58 mmol, 1.0 eq) in NMP (2 mL) was added N,N-diisopropylethylamine (0.38 mL, 2.3 mmol, 4.0 eq) and the reaction mixture heated to 100 C for 1 hr. In some cases, lower temperatures or longer reaction times were used. The reaction mixture was cooled, diluted heavily with EtOAc, and washed repeatedly with brine (3x). The organic layer was dried over Na2SC>4 and concentrated. Silica gel column (24 g) was loaded using methylene chloride and run using an increasing gradient of MeOH (0-20%) in methylene chloride over 20 min to provide (2R)-4-(4-ainino-5-cyanopyrimidin-2-yl)-N-[2-(l-benzylpiperidin-4-yl)ethyl]-2- methylpiperazine-l-carboxamide 5-1 (0.14 g, 0.31 mmol, 53%) as an off-white foam.
The chemical industry reduces the impact on the environment during synthesis 94741-69-2, I believe this compound will play a more active role in future production and life.
Reference:
Patent; NEUROCRINE BIOSCIENCES, INC.; HARRIOTT, Nicole; PAGANO, Nicholas; (135 pag.)WO2017/79641; (2017); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia