Mitratapide, R-103757

米瑞他匹Chemical Name: 4-[4-[4-[4-[(2S,4R)-2-(4-Chlorophenyl)-2-(4-methyl-4H-1,2,4-triazol-3-ylsulfanylmethyl)-1,3-dioxolan-4-ylmethoxy]phenyl]piperazin-1-yl]phenyl]-2-[1(R)-methylpropyl]-2,4-dihydro-3H-1,2,4-triazol-3-one
CAS No. 179602-65-4, 179602-63-2 (diastereomer), 248584-97-6 (diastereomer)
项目整合开发状态: Preclinical
项目研究机构: Janssen (Originator)
合成路线:Bromoacetophenone (I) was converted into a cis/trans mixture of ketals (III) by treatment with glycerin (II) and p-toluenesulfonic acid.Subsequent reaction of (III) with 2-naphthalenesulfonyl chloride gave the corresponding mixture of sulfonate esters.After separation of the desired cis-isomer (IV),its condensation with the phenol derivative (V) produced ether (VI).Finally,displacement of the bromine atom of (VI) with 3-mercapto-4-methyl-1,2,4-triazole (VII) using Na2CO3 in DMF gave rise to the title thioether.