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【结 构 式】

【药物名称】NOBEX-AA-004, NAA-004, APAZA

【化学名称】5-[4-(Carboxymethyl)phenyldiazenyl]-2-hydroxybenzoic acid

【CA登记号】

【 分 子 式 】C15H12N2O5

【 分 子 量 】300.27329

【开发单位】Nobex (Originator)

【药理作用】Chemical Delivery Systems, DRUG DELIVERY, Drug Delivery Systems, GASTROINTESTINAL DRUGS, IMMUNOMODULATING AGENTS, Immunomodulators, Inflammatory Bowel Disease, Agents for

合成路线1

The diazotization of 2-(4-aminophenyl)acetic acid (I) by means of NaNO2 and HCl gives the diazonium salt (II), which is then condensed with 2-hydroxybenzoic acid (III) to provide the target azocompound.

1 Riggs-Sauthier, J.A.; Malson, E.; Harris, M.; Myung, S.; Liddle, R.; Ekwuribe, N.; Synthesis and activity of novel 5-aminosalicylic acid (5-ASA)-containing prodrugs for the treatment of inflammatory bowel disease. 224th ACS Natl Meet (Aug 18 2002, Boston) 2002, Abst MEDI 305.
2 Ekwuribe, N.N.; Riggs-Sauthier, J. (Nobex Corp.); Immunoregulatory cpds. and derivs. and methods of treating diseases therewith. WO 0218324 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 21229 2-(4-Aminophenyl)acetic acid 5345-54-0 C8H9NO2 详情 详情
(II) 55812 4-(carboxymethyl)benzenediazonium chloride C8H7ClN2O2 详情 详情
(III) 15240 2-Hydroxybenzoic acid; Salicylic acid 69-72-7 C7H6O3 详情 详情
Extended Information