BN-80933

N1-[4-[4-[6-羟基-2,5,7,8-四甲基-3,4-二氢-2H-1-苯并哋-2(S)-羰基]哌嗪-1-基]苯基]噻吩-2-羧脚Chemical Name: N1-[4-[4-[6-Hydroxy-2,5,7,8-tetramethyl-3,4-dihydro-2H-1-benzopyran-2(S)-ylcarbonyl]piperazin-1-yl]phenyl]thiophene-2-carboxamidine
CAS No. 214348-10-4, 214124-18-2 (undefined isomer)
项目整合开发状态: Preclinical
项目研究机构: Ipsen (Originator)
合成路线:(S)-6-Hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid (I) was coupled to N-(4-nitrophenyl)piperazine (II) via activation with 1,1'-carbonyldiimidazole to furnish the corresponding amide (III).Subsequent hydrogenation of the nitro group of (III) over Pd/C provided aniline (IV).This was finally condensed with S-methyl-2-thiophenethiocarboxamide (V) to yield the title amidine.

合成路线:2-thiophenecarbonitrile (VI) was converted into imidate (VII) and then coupled with aniline (IV) in refluxing MeOH to give the title compound.