NO-Mesalamine, NO-5-ASA, NCX-456

Chemical Name: 5-Amino-2-hydroxybenzoic acid 4-(nitrooxy)butyl ester
CAS No. 256499-26-0
项目整合开发状态: Preclinical
项目研究机构: NicOx (Originator)
合成路线:5-Amino-2-hydroxybenzoic acid (I) was protected as the N-Boc derivative (II) by treatment with di-tert-butyl dicarbonate and Et3N.Reaction with triphenylphosphine and carbon tetrabromide in tetrahydrofuran generated the bromobutyl ester (III).After conversion of (III) to the nitroxybutyl ester (IV) by reaction with AgNO3 in refluxing acetonitrile,acid deprotection of the Boc group furnished the title compound.