Method for preparing 4-amino-3-(4-aminobenzene)furo[2,3-d] pyrimidine

Abstract

The invention discloses a method for preparing 4-amino-3-(4-aminobenzene)furo[2,3-d] pyrimidine. The method comprises the following steps: using nitroacetophenone as a raw material, reacting the nitroacetophenone and N-bromo-succinimide to generate 2-bromo-1-(4-nitrophenyl)aceton by using para-toluenesulfonic acid as a catalyst, further reacting the 2-bromo-1-(4-nitrophenyl)aceton, sodium acetate and tetrabutylammonium bromide to generate 2-acetoxyl-1-(4-nitrophenyl)aceton, through reducing nitro into amino, reacting the 2-bromo-1-(4-nitrophenyl)aceton and hydrochloric acid, and reducing acetoxyl group into hydroxy to obtain 1-(4-aminophenyl)-2-hydroxy-aceton; then reacting the 1-(4-aminophenyl)-2-hydroxy-aceton, malononitrile and diethylamine to obtain 2-amino-4-(4-aminophenyl)-3-furan nitrile; finally reacting the 2-amino-4-(4-aminophenyl)-3-furan nitrile and formamidine acetate to obtain the 4-amino-3-(4-aminobenzene)furo[2,3-d] pyrimidine. The method has the advantages that the operation is simple and the total recovery is high.

Description

technical field [0001] The invention belongs to the field of chemistry, and in particular relates to a pharmaceutical intermediate 4-amino-3-(4-aminobenzene)furo[2,3-d]pyrimidine, specifically a method for preparing 4-amino-3-( 4-aminophenyl)furo[2,3-d]pyrimidine method. [0002] Background technique [0003] Animal experiments have shown that furo[2,3-d]pyrimidine derivatives, as receptor-interacting protein 1 (RIP1) enzyme inhibitors, have good curative effects on diseases related to cell necrosis, such as: brain, retina and kidney defects Blood / reperfusion injury, myocardial infarction, retinal detachment, inflammation, gastrointestinal and skin diseases, etc. Therefore, furo[2,3-d]pyrimidine derivatives play an important role in future pharmaceutical research and development. [0004] For the synthesis of furo[2,3-d]pyrimidine derivatives——4-amino-3-(4-aminobenzene)furo[2,3-d]pyrimidine, the following methods have been reported in the literature, but all There are th...

AI Technical Summary

Problems solved by technology

[0015] Aiming at the above-mentioned technical problems in the above-mentioned prior art, the present invention provides a method for preparing 4-amino-3-(4-aminobenzene)furo[2,3-d]pyrimidine, the preparation method Solve the technical problems of complex preparation process, low yield and serious environmental pollution in the prior art

Images