These common heterocyclic compound, 138642-47-4, name is 2-Bromo-5-methoxybenzonitrile, 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. name: 2-Bromo-5-methoxybenzonitrile
Step A: KOH (4M, 259.66uL, 3.06eq) and Pd(Ph3P)2Cl2 (47.65mg, 67.88umol, 0.20eq) were added to a solutionof the intermediate 12 (200.00mg, 339.42umol, 1.00eq) and 2-bromo-5-methoxyphenyl cyanide (108.00mg, 509.13umol,1.50eq) in 2-methyltetrahydrofuran. The reaction solution was stirred at 65C under nitrogen atmosphere for 13 hours,then cooled to room temperature, and additional Pd(Ph3P)2Cl2 (20.00mg, 33umol, 0.10eq) was added. The reactionsolution was heated to 65C and stirred for another 3 hours to give 87, which was directly used in the next step. Thereaction solution was cooled to room temperature, then methanol (6.00mL) and water (3.00mL) were added and theresulting mixture was stirred at 35C for 2 hours. Lithium hydroxide (15mg) was added, the reaction solution was heatedto 45C and stirred for 3 hours. The reaction solution was cooled to room temperature, adjusted to pH 5 with 2M HCl,diluted with water, extract with ethyl acetate, dried over sodium sulfate, concentrated and purified by silica gel columnchromatography to give the intermediate 88.
The synthetic route of 2-Bromo-5-methoxybenzonitrile has been constantly updated, and we look forward to future research findings.