Reference of 25017-13-4, A common heterocyclic compound, 25017-13-4, name is 1-(2-Bromoethyl)-3-fluorobenzene, molecular formula is C8H8BrF, 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.
To 2-(9-oxa-3,7-diaza-bicyclo[3.3.1]non-3-yl)-ethanesulfonic acid 4-cyano- benzylamide dihydrochloride (0.127 g, 0.30 mmol; prep P above), 1-(2- bromo-ethyl) -3-fluoro-benzene (0.064 g, 0.315 mmol) and potassium carbonate (0.145 g, 1.05 mmol) was added acetonitrile (4 mL) and water (0.1 mL). The mixture was stirred for 20 minutes before it was heated by microwave irradiation (10 minutes, 160C) and was then filtered and evaporated. The crude product was purified by chromatography on silica gel using methanol saturated with ammonia in dichloromethane as eluent, which afforded 43 mg (30.3%) of the title compound. ยน3C NMR (125.7 MHz, CDCl3) 8 163.90,161.94, 144.35,141.66, 132.65, 130.03,129.96, 128.11,123.86, 118.70,115.12, 114.95,113.51, 113.34, 111.76, 68.34, 60.85, 56.85, 56.41, 54.40, 47.82, 47.47, 31.35
The synthetic route of 25017-13-4 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; ASTRAZENECA AB; WO2005/123748; (2005); A1;,
Bromide – Wikipedia,
bromide – Wiktionary