SSR-146977

N'-[1-[3-[(3R)-1-苯甲酰基-3-(3,4-二氯苯基)-3-哌啶基]丙基]-4-苯基-4-哌啶基]-N,N-二甲基脲Chemical Name: N-[1-[3-[1-Benzoyl-3(R)-(3,4-dichlorophenyl)piperidin-3-yl]propyl]-4-phenylpiperidin-4-yl]-N',N'-dimethylurea
CAS No. 264618-44-2, 264618-48-6 (benzoate), 264618-45-3 (fumarate), 264618-38-4 (hydrochloride), 264618-47-5 (succinate), 264618-49-7 (undefined stereoch.)
项目整合开发状态: Phase I
项目研究机构: Sanofi-Aventis (Originator)
合成路线:Acidic hydrolysis of 4-acetylamino-1-benzyl-4-phenylpiperidine (I) gives diamine (II).Subsequent acylation of (II) with dimethylcarbamoyl chloride affords urea (III).The N-benzyl protecting group is then removed by catalytic hydrogenolysis over Pd/C to furnish piperidine (IV)

合成路线:The previously reported (hydroxypropyl)piperidine derivative (V) is subjected to Swern oxidation to produce aldehyde (VI).Then,reductive amination of (VI) with piperidine (IV) in the presence of NaBH3CN affords the target compound