A green synthetic method for tert-butyl bromoacetate

Abstract

The invention relates to a green synthetic method for tert-butyl bromoacetate. The method is characterized in that bromoacetic acid and isobutylene are adopted as raw materials in the method, a solid superacid is adopted as a catalyst, and the method includes performing an acid-ester esterification reaction at room temperature under atmospheric pressure in an organic solvent, performing filtration after the reaction is finished to recover the catalyst, distilling filtrate to recover the solvent and distilling to obtain the tert-butyl bromoacetate the content of which is 99.0% or above. The reaction yield is 95% or above. The method is high in yield, good in product quality, low in cost, simple in reaction process operation, basically free of generation of three wastes, low in environment pollution, high in operation safety and suitable for industrial production. The catalyst is easily available and can be used repeatedly.

Description

technical field [0001] The invention belongs to the field of synthesis and preparation of pharmaceutical intermediates, in particular to a green synthesis method of tert-butyl bromoacetate. Background technique [0002] Tert-butyl bromoacetate is a light yellow transparent liquid, soluble in alcohol, ether and other organic solvents, used for the synthesis of amino acids and peptide compounds, and is used for the synthesis of cyclic polyamine polycarboxylate contrast agents, cephalosporins, It is an important intermediate of drugs such as receptor antagonists and a common alkylating agent. [0003] There are few domestic production enterprises of tert-butyl bromoacetate, especially there are almost no enterprises with large output, which makes the country have to rely on imports to meet demand, which largely restricts the development of tert-butyl bromoacetate in my country. [0004] There are few reports on the synthesis of tert-butyl bromoacetate in China. "The Simple Syn...

AI Technical Summary

Problems solved by technology

The bromoacetyl chloride used in this route is more toxic, and there are many side reactions in the reaction, which is difficult to separate from the product, and the content of the product obtained is low, and the yield is low

Reaction equipment and production process require harsh conditions, thionyl chloride severely corrodes the equipment, produces a large amount of waste water and waste gas, and is difficult to treat. The used fuacid is very polluting to the environment, high in cost, labor-intensive, and cumbersome in post-processing. , it is difficult to form large-scale production, and there are great safety hazards in production