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Hydroxybenzoyl Chlorides in the Synthesis of Conjugates with Biologically Active Dipeptides
Russian Journal of Organic Chemistry ( IF 0.8 ) Pub Date : 2021-05-24 , DOI: 10.1134/s1070428021040060
A. K. Brel , S. V. Lisina , Yu. N. Budaeva

Abstract

Conjugates of hydroxy- and acetoxybenzoic acids with dipeptides based on 4-aminobutanoic acid and glycine were synthesized through hydroxy(acetoxy)benzoyl chlorides and 4-[hydroxy(acetoxy)benzoyl­amino]butanoyl chlorides as intermediate products. Acyl chlorides were prepared by treatment of the corre­sponding acids with oxalyl chloride in the presence of dimethylformamide at a ratio of 1:1.1:0.07 in boiling benzene. The target N-[hydroxy(acetoxy)benzoyl] derivatives of dipeptides were obtained with high yields, and no further purification of the products was necessary. The synthesized compounds were evaluated as potential neuroprotective agents.



中文翻译:

具有生物活性二肽缀合物的羟基苯甲酰氯的合成

摘要

通过羟基(乙酰氧基)苯甲酰氯和4- [羟基(乙酰氧基)苯甲酰氨基]丁酰氯作为中间产物,合成了羟基和乙酰氧基苯甲酸与基于4-氨基丁酸和甘氨酸的二肽的缀合物。通过在二甲基甲酰胺存在下,在沸腾的苯中以1:1.1:0.07的比例用草酰氯处理相应的酸来制备酰氯。高产率地获得二肽的目标N- [羟基(乙酰氧基)苯甲酰基]衍生物,并且不需要进一步纯化产物。评价合成的化合物作为潜在的神经保护剂。

更新日期:2021-05-24
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