Lobenzarit sodium, CCA, Carfenil

氯苯扎利二钠 2-((2-羧基苯基)氨基)-4-氯苯甲酸 Chemical Name: 4-Chloro-2,2'-iminidibenzoic acid disodium salt
CAS No. 64808-48-6, 63329-53-3 (free acid)
项目整合开发状态: Launched-1986
项目研究机构: Chugai (Originator)
合成路线:By condensation of 2,4-dichlorobenzoic acid (I) with anthranilic acid (II) by means of K2CO3,powdered Cu and a small amount of I2 in refluxing isoamyl alcohol.

合成路线:Condensation of 2-acetylthiophene (I) with dimethylformamide dimethylacetal produced enaminone (II),which was subsequently cyclized to the isoxazole (III) upon treatment with hydroxylamine.Further condensation of (III) with dimethylformamide dimethylacetal,with concomitant isoxazole ring opening,gave rise to the enamino nitrile (IV).This was then cyclized with aminoguanidine nitrate (V) under basic conditions to furnish the intermediate aminopyrazole (VI).

合成路线:3-(Acetamido)acetophenone (VII) was converted to enaminone (VIII) upon condensation with dimethylformamide dimethylacetal.The amide N of (VIII) was then alkylated by means of iodomethane and NaH or,alternatively,under phase-transfer conditions to give (IX).Finally,condensation between enaminone (IX) and aminopyrazole (VI) in refluxing AcOH provided the target pyrazolopyrimidine.