Method for preparing 2-bromo-fluorobenzyl bromide

Abstract

The invention relates to the field of organic synthesis, in particular to a method for preparing 2-bromo-fluorobenzyl bromide, which comprises the following steps: (1) in the presence of an organic or inorganic solvent, adding a 2-bromo-6-fluorotoluene compound and 40-mass-percent hydrobromic acid and dripping 30-mass-percent hydrogen peroxide under a lighting condition, and reacting for 6 to 24 hours, wherein the molar ratio of 2-bromo-6-fluorotoluene to HBr is 1:(1-3.5) and the molar ratio of the 2-bromo-6-fluorotoluene to H2O2 is 1:(1-3.5); and (2) washing the reaction solution with saturated sodium sulfite solution and water, drying the reaction solution with anhydrous sodium sulfate, evaporating solvent under a reduced pressure, and obtaining the 2-bromo-6-fluorotoluene compound by silica gel column chromatography. In the method, the hydrobromic acid and hydrogen peroxide are used in place of the traditional N-bromosuccinimide brominating agent, so the production cost is reduced; and lighting is used in place of a benzoyl peroxide initiator, so method has the advantages of mild reaction conditions, high product purity, high yield and the like.

Description

technical field

[0001] The invention relates to the field of organic synthesis, in particular to a method for preparing 2-bromo-6-fluorobenzyl bromide through bromination reaction. The invention provides a simple and economical method for preparing 2-bromo-6-fluorobenzyl bromide. Background technique

[0002] 2-Bromo-6-fluorobenzyl bromide is an important pharmaceutical intermediate. In the patent WO2007031828A2, Fluoxetine was synthesized from 2-bromo-6-fluorobenzyl bromide. The trade name is “Bioyoujie” Or "Prozac" (Prozac), is a drug developed by Eli Lilly and Company for the treatment of adult depression, obsessive-compulsive disorder and bulimia nervosa; patent WO2005059107A2 uses 2-bromo-6-fluorobenzyl bromide Piperidine derivatives synthesized as raw materials can be used to inhibit HIV virus; gram crown acid sodium synthesized from 2-bromo-6-fluorobenzyl bromide in patent WO03066620A1 can be used to treat angina pectoris, unstable sore throat and other diseases; pat...