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ChemicalBook CAS DataBase List 4-AMINO-2-METHYLPYRIMIDINE-5-CARBONITRILE

4-AMINO-2-METHYLPYRIMIDINE-5-CARBONITRILE synthesis

11synthesis methods
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Yield: 92.6%

Reaction Conditions:

Stage #1:formaldehyd;acetamidine hydrochloride;malononitrile in water;tert-butyl alcohol at 65 - 70; for 4 h;Mannich Aminomethylation;
Stage #2: with tert.-butylhydroperoxide in water;tert-butyl alcohol at 20 - 35; for 1 h;Temperature;Solvent;Reagent/catalyst;

Steps:

2 Example 2: Preparation of 2-methyl-4-amino-5-cyanopyrimidine
To a 50 ml three-necked flask equipped with a magnetic stirrer, a thermometer and a reflux condenser were added 10 g of t-butanol,1.13 g (12 mmol) of acetamidine hydrochloride, 0.66 g (0.1 mol) of malononitrile and 1.2 g (12 mmol) of 30% aqueous formaldehyde were added, and the mixture was reacted at 65-70 ° C for 4 hours.Cooled to 20 ~ 25 ° C, 1.4 g of 70wt% t-butylperoxy peroxide was added and the reaction was carried out at 30-35 ° C for 1 hour. Samples were taken and detected by external standard method. The product 2-methyl-4-amino-5-cyanopyrimidine The yield was 92.6% and the HPLC purity was 99.6%.

References:

Xin Fa Pharmaceutical Co., Ltd.;Qi Yuxin;Wang Likai;Wang Jingcheng;Zhu Chengchen;Yu Dawei;Ju Lizhu;Li Xinfa CN106279042, 2017, A Location in patent:Paragraph 0041; 0042; 0043; 0044; 0045; 0046; 0047-0052

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