Synthetic Route of 202865-83-6, These common heterocyclic compound, 202865-83-6, name is 1-Bromo-3-fluoro-5-methylbenzene, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
Step 1: Preparation of 8-(3-fluoro-5-methyl-phenyl)-1,4-dioxa-8-azaspiro[4.5]decane A mixture of 1,4-dioxa-8-azaspiro[4.5]decane hydrochloride (4.0 g, 22.3 mmol), 1-bromo- 3-fluoro-5-methylbenzene (5.05 g, 26.7 mmol), Pd2(dba)3 (408 mg, 445 mumol), Ruphos (416 mg, 891 mumol) and Cs2CO3 (18.1 g, 55.7 mmol) in toluene (50 mL) was heated with stirring at 120 C for 15 hrs. The resulting reaction mixture was filtered through celite and the filtrate was concentrated in vacuo. The residue was purified by flash chromatography to give 8-(3-fluoro-5- methyl-phenyl)-1,4-dioxa-8-azaspiro[4.5]decane (5.0g) as a yellow oil.
Statistics shows that 1-Bromo-3-fluoro-5-methylbenzene is playing an increasingly important role. we look forward to future research findings about 202865-83-6.
Reference:
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; CHENG, Zhanling; HAN, Xingchun; JIANG, Min; WANG, Jianhua; WANG, Min; WANG, Yongguang; YANG, Song; (319 pag.)WO2016/177655; (2016); A1;,
Bromide – Wikipedia,
bromide – Wiktionary