TBC-3711

N-(2-乙酰基-4,6-二甲基苯基)-3-[[(3,4-二甲基-5-异恶唑基)氨基]磺酰基]-2-噻吩甲酰胺Chemical Name: N-(2-Acetyl-4,6-dimethylphenyl)-3-[N-(3,4-dimethylisoxazol-5-yl)sulfamoyl]thiophene-2-carboxamide
CAS No. 349453-49-2, 374680-51-0, 349453-84-5 (sodium salt)
项目整合开发状态: Phase I
项目研究机构: Encysive Pharmaceuticals (Originator)
合成路线:Coupling between 2-(methoxycarbonyl)-3-thiophenesulfonyl chloride (I) and 5-amino-3,4-dimethylisoxazole (II) afforded the corresponding sulfonamide (III).The sulfonamide NH group of (III) was then protected by reaction with bromomethyl methyl ether to produce the methoxymethyl derivative (IV).Basic hydrolysis of the methyl ester function of (IV),followed by treatment of the resultant carboxylic acid (V) with oxalyl chloride,furnished the acid chloride (VI).This was then coupled with 2'-amino-3',5'-dimethylacetophenone (VII) to yield amide (VIII).The methoxymethyl protecting group of (VIII) was finally removed by acidic treatment to provide the title compound.