YM-91746

Chemical Name: N-[6-Methoxy-5-(2-methoxyphenoxy)-2,2'-bipyrimidin-4-yl]-1-phenyl-1(E)-butene-2-sulfonamide potassium salt
CAS No. 192645-50-4 (undefined isomer)
项目整合开发状态: Preclinical
项目研究机构: Yamanouchi (Originator)
合成路线:The known dichloropyrimidine derivative (I) was condensed with 2-phenylethenesulfonamide (II) in the presence of NaH in DMF to furnish the N-pyrimidinylsulfonamide (III).Displacement of the remaining chlorine of (III) by means of methanolic NaOMe provided the corresponding methyl ether (IV).The title potassium salt was then prepared by treatment of sulfonamide (IV) with ethanolic KOH.

合成路线:Nucleophilic substitution of the dichloropyrimidine derivative (I) with 2-phenylvinylsulfonamide (II) in the presence of NaH in DMF affords the sulfonamido pyrimidine (III).The remaining chloro group of (III) is subsequently displaced with the sodium alkoxide derived from 2-fluoroethanol (IV) to provide the target fluoroethyl ether.

合成路线:The sulfonation of 1-phenyl-1-butene (I) with sulfuryl chloride in hot DMF provided sulfonyl chloride (II),which was then treated with ammonium hydroxyde to give sulfonamide (III).Coupling of the known dichloro bipyrimidinyl derivative (IV) with the sodium salt of sulfonamide (III) yielded the N-pyrimidinyl sulfonamide (V).The remaining chloride was then displaced with sodium methoxide in DMF,and the resultant sulfonamide was finally converted to the potassium salt with ethanolic KOH.