Susalimod

2-羟基-5-[2-[4-[(3-甲基吡啶-2-基)氨基磺酰基]苯基]乙炔基]苯甲酸Chemical Name: 2-Hydroxy-5-[4-[N-(3-methyl-2-pyridyl)sulfamoyl]phenylethynyl]benzoic acid
CAS No. 149556-49-0
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:Palladium-catalyzed coupling of methyl 5-iodosalycilate (I) with trimethylsilyl acetylene (II) produced the ethynyl salycilate (III).The trimethylsilyl protecting group of (III) was then cleaved by treatment with KF in DMF to give (IV).On the other hand,sulfonamide (VII) was obtained by condensation of 4-iodobenzenesulfonyl chloride (V) with 2-amino-3-methylpyridine (VI).A further Suzuki coupling between acetylene (IV) and iodosulfonamide (VII) furnished diaryl acetylene (VIII).The methyl ester group of (VIII) was finally saponified with NaOH to provide the target carboxylic acid.