Electric Literature of 591-55-9, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 591-55-9, name is 5-Aminopyrimidine, molecular formula is C4H5N3, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.
A solution of X-Phos (0.04 equiv) and Pd2(dba)3 (0.02 equiv) in toluene (15 vol) was bubbled with nitrogen and heated to 60 C for 15 min. (2S,4R)-1-(2-(3-acetyl-5-bromo-1H-indol-1-yl)acetyl)-4-fluoro-N-(4-phenylbutyl)pyrrolidine-2-carboxamide (1 equiv), 5- aniinopyriniidine (1.2 equiv) and sodium tert-butoxide (1.4 equiv) was added to the reaction mixture and the reaction mixture was heated to 100 C for 16 h. After completion of the reaction, the reaction mixture was quenched with water. The resulting mixture was extracted with ethyl acetate. The organic layer was separated, dried over anhydrous Na2S04, filtered and then concentrated. The residue was purified by column chromatography on silica gel using DCM/MeOH to give (2S,4R)-1-(2-(3-acetyl-5-(pyrimidin-5-ylamino)-1H-indol-1-yl)acetyl)-4-fluoro-N-(4-phenylbutyl)pyrrolidine-2-carboxamide. H NMR (400 MHz, DMSO-d6) delta 8.57 (s, 1H), 8.48 – 8.45 (m, 3H), 8.22 (s, 1H), 8.02 – 8.00 (m, 2H), 7.43 (d, J = 8.8 Hz, 1H), 7.19 – 7.05 (m, 5H), 5.56 – 5.32 (m, 2H), 5.15 (d, J= 17.1 Hz, 1H), 4.38 – 4.34 (m, 1H), 4.16 – 4.11 (m, 1H), 3.95 – 3.83 (m, 1H), 3.07 – 2.99 (m, 4H), 2.40 (s, 3H), 2.38 – 2.34 (m, 1H), 2.01 – 1.98 (m, 1H), 1.56 – 1.48 (m, 2H), 1.41 – 1.33 (m, 2H).
While traditionally a conservative industry, chemical producers will need to modernize their PR strategies to stay relevant.we look forward to future research findings about 591-55-9, 5-Aminopyrimidine.
Reference:
Patent; ACHILLION PHARMACEUTICALS, INC.; WILES, Jason, Allan; PHADKE, Avinash, S.; DESHPANDE, Milind; AGARWAL, Atul; CHEN, Dawei; GADHACHANDA, Venkat, Rao; HASHIMOTO, Akihiro; PAIS, Godwin; WANG, Qiuping; WANG, Xiangzhu; (319 pag.)WO2017/35351; (2017); A1;,
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