SZ-042

Chemical Name: 1-(4-Amino-2-methylquinazolin-6-yl)-N-[-3-fluoro-2'-(sulfamoyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线:The condensation of diketone (I) with hydrazine (II) in refluxing EtOH gave pyrazole (III).Carboxylic acid (IV) was then obtained by oxidative cleavage of the furan ring with KMnO4.After conversion of (IV) to the corresponding acid chloride (V),coupling with the biphenyl amine (VI) provided amide (VII).Ring closure of the fluoronitrile group with acetamidine hydrochloride (VIII) with concomitant deprotection of the N-tert-butyl group furnished the title aminoquinazoline derivative.