| 参考文献No. | 43061 |
| 标题: | Ureidopiperidine derivs. as selective human NK3 receptor antagonists |
| 作者: | Proietto, V.; Van Broeck, D.; Edmonds-Alt, X.; Aulombard, A. (Sanofi-Synth閘abo) |
| 来源: | EP 1119552; JP 2002527423; US 6465489; WO 0021931 |
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| 合成路线图解说明: 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) |
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| 合成路线图解说明: 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 |