Synthetic Route of 428854-24-4, 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.428854-24-4, name is 2-(1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)pyrimidine-4,5,6-triamine, molecular formula is C17H15FN8, molecular weight is 350.35, as common compound, the synthetic route is as follows.
Step three, A solution of formic acid (129 g, 1.37 mol)Was added dropwise to acetic anhydride (145 g, 1.42 mol)After stirring for half an hour, compound 4 (80 g, 0.23mo 1) was added at 0 C, stirred at 20 C for 10 hours,TLC detection reaction is completed, concentrated reaction solution, add 500mL of water for half an hour, pumping,Dried to give about 78 g of a yellow solid which was dissolved in 500 mL of tetrahydrofiramidate and sodium borohydride (15.58 g, 0.41 mol) was added at room temperature. A solution of boron trifluoride diethyl ether (90 mL) was slowly added dropwise at room temperature, Slowly heated to reflux for 3 hours. After the reaction, add 120mL methanol to destroy, then add 2N hydrochloric acid 120mL, stir for half an hour after the reaction system, the residue with 2N sodium hydroxide solution to adjust the pH to neutral, and then suction, Drying to obtain a crude product of compound 5a,The crude product of compound 5a was dissolved in a mixed solvent of dichloromethane and methanol (the weight ratio of the crude product of compound 5a to 1: 5, the volume ratio of dichloromethane to methanol in the mixed solvent was 1: 15) ,And the mixture was stirred at room temperature for 10 hours and then filtered and dried to obtain pure product (63.7 g, 0.17 mol, yield: 76%, content: 99%) /
The chemical industry reduces the impact on the environment during synthesis 428854-24-4, I believe this compound will play a more active role in future production and life.
Reference:
Patent; Anhui Lianchuang Biological Medicine Co.,Ltd; GE, DEPEI; WU, QIHUA; LIU, TAO; (10 pag.)CN104530044; (2016); B;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia