Application of 51376-06-8, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 51376-06-8, name is 5-Bromobenzo[c][1,2,5]oxadiazole belongs to bromides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.
l-(2-((2S,4R)-4-Fluoro-2-((2-fluoro-3-(4,4,5,5-tetramethyl-l,3,2-dioxaborolan-2- yl)phenyl)carbamoyl)pyrrolidin-l-yl)-2-oxoethyl)-lH-indazole-3-carboxamide, 5- bromobenzo[c][l,2,5]oxadiazole, Pd(dppf)Cl2 and potassium carbonate were taken up in a pressure tube under argon. To this mixture, 8 mL of dioxane and 2 mL of water were added. The mixture was bubbled with argon for 5 min and the vial was stoppered and subjected to microwave irradiation at 100 C for 45 min. The volatiles were removed under reduced pressure and the residue was purified by ISCO (0-5 % MeOH in CH2CI2) to afford compound 68. 1HNMR (400 MHz, DMSO) (major rotamer) delta 2.10 – 2.20 (m, 1H), 2.57-2.63 (m, 1H), 3.89 – 4.04 (m, 1H), 4.24 (dd, J = 12.7, 21.8 Hz, 1H), 4.78 (t, J = 8.3 Hz, 1H), 5.47 (d, J= 17.2 Hz, 1H), 5.55 (d, J = 52.4 Hz, 1H), 5.67 (d, j = 17.2 Hz, 1H), 7.23-7.31 (m, 2H), 7.36 (s, 1H), 7.39 – 7.46 (m, 2H), 7.59 – 7.64 (m, 2H), 7.74 (d, J= 9.3 Hz, 1H), 7.98 (t, J= 7.8 Hz, 1H), 8.11 – 8.25 (m, 3H), 10.05 (s, 1H). 19F- MR (DMSO-de ) (major rotamer): delta -128.8, -175.9.
The synthetic route of 5-Bromobenzo[c][1,2,5]oxadiazole has been constantly updated, and we look forward to future research findings.
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; GREENLEE, William; (447 pag.)WO2017/35408; (2017); A1;,
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