128038-37-9

Upstream product

• 18197-26-7 sodium diformamide 
• 589-17-3 p-bromobenzyl chloride 
• 589-15-1 1-bromomethyl-4-bromobenzene 

Downstream Products

• 26177-44-6 4-bromobenzylamine hydrochloride 

Relevant academic research and scientific papers

A Convenient Synthesis of Primary Amines Using Sodium Diformylamide as A Modified Gabriel Reagent

Sodium diformylamide (1) was used as a convenient substitute for phthalimide in the Gabriel synthesis of primary amines.Reagent 1 undergoes smooth N-alkylation with alkyl halides or p-toluenesulfonates 2 in acetonitrile or dimethylformamide to give the corresponding N,N-diformylalkylamines 3 in good yields, except with alkylating agents which are susceptible to base-catalyzed elimination.The formyl group of 3 can be easily removed by hydrochloric acid to give the corresponding alkylamine hydrochlorides 5 or free alkylamines 4.

Preparation method of intermediate p-bromobenzylamine hydrochloride for synthesizing protein degradation agent 1

The invention discloses a preparation method of an intermediate p-bromobenzylamine hydrochloride for synthesizing a protein degradation agent 1, which comprises the following steps: sequentially adding a certain amount of p-bromobenzyl bromide, sodium diformylamide and an ether inert solvent, conducting reacting for 10-15 hours at a certain temperature, cooling the reaction system to room temperature, and conducting filtering to obtain filtrate; concentrating the filtrate under reduced pressure to remove the solvent to obtain a residue, sequentially adding a certain amount of ethanol and concentrated hydrochloric acid into the residue, conducting reacting for 15-20 hours at a certain temperature, and cooling a formed reaction system to room temperature; and then adding a certain amount of ethyl acetate for crystallization, and conducting filtering and drying to obtain the p-bromobenzylamine hydrochloride. According to the synthesis method of the p-bromobenzylamine hydrochloride, dangerous chemicals sodium azide and hydrazine hydrate used in preparation of the p-bromobenzylamine hydrochloride reported in existing literatures are avoided, meanwhile, the three wastes are few, the yield is high, and the synthesis method has the advantages of being easy to operate, high in safety, good in product quality, low in cost and the like and is convenient for large-scale production.