新产品编号:2311811
Chemical Name: 2,2-Dimethylpropionic acid 3-[2-[4-(2-aminoethoxy)-3-methoxyphenyl]acetamido]-2-(3,4-dimethylbenzyl)propyl ester
项目整合开发状态: Preclinical
项目研究机构: AmorePacific (Originator), National Cancer Institute (Originator), Seoul National University (Originator)
合成路线:Hydrogenation of the previously reported azide (I) over Lindlar's catalyst produces amine (II),which is subsequently acylated by homovanillic acid pentafluorophenyl ester (III),yielding amide (IV).Alkylation of the phenolic hydroxyl of (IV) with 1,2-dibromoethane under phase-transfer conditions leads to the bromoethyl ether (V).Displacement of bromide (V) with NaN3 gives the alkyl azide (VI).The azido group of (VI) is finally reduced to the desired amine by catalytic hydrogenation over Pd/C.
📌 参考资料/链接:
参考文献标题:Phenolic modification as an approach to improve the pharmacology of the 3-acyloxy-2-benzylpropyl homovanillic amides and thioureas,a promising class of vanilloid receptor agonists and analgesics
文献作者:Lee,J.; Kang,M.-S.; Kim,K.-P.; Chung,S.-J.; Blumberg,P.M.; Yi,J.-B.; Park,Y.H.
参考来源:Bioorg Med Chem 2002,10(4),1171