A-285354.0

N-[4-[3,5-双(三氟甲基)-1H-吡氮卓-1-酰基]-3-氟苷-4-羧酰胺Chemical Name: N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoropyridine-4-carboxamide
CAS No. 245747-08-4
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator), Millennium (Originator)
合成路线:Acid-catalyzed condensation of 4-nitrophenylhydrazine (I) with 1,1,1,5,5,5-hexafluoro-2,4-pentanedione (II) produced pyrazole (III).Reduction of the nitro group of (III) to the corresponding amine (IV) was achieved either by treatment with stannous chloride or by catalytic hydrogenation over Pd/C.Fluoroisonicotinic acid (VI) was prepared by lithiation of 3-fluoropyridine (V) at -78 C followed by quenching with dry ice.Finally,coupling of acid (VI) with amine (IV) yielded the target amide.