4-piperidinylamine; 4-piperidinamine; 4-aminopiperidine -Drug Synthesis Database

【结构式】

【分子编号】17502

【品名】4-piperidinylamine; 4-piperidinamine; 4-aminopiperidine

【CA登记号】13035-19-3

【分子式】C₅H₁₂N₂

【分子量】100.16376

【元素组成】C 59.96% H 12.08% N 27.97%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号：(II)

Norastemizole can be obtained in the following way as shown in scheme: The synthesis is carried out by mild and selective palladium coupling of readily available 1-(4-fluorobenzyl)- 2-chlorobenzimidazole (I) with 4-aminopiperidine dihydrochloride (II) to obtain norastemizole in 84% isolated yield. The synthesis is highly selective and involves a one-step process.

参考文献中间体

合成目标

【1】 Xiang, T.; Hong, Y.; Wald, S.A.; Tanoury, T.; Senanayake, C.H.; Vandenbossche, C.P.; Bakale, R.P.; Remarkably Selective Palladium-Catalyzed Amination Process: Rapid Assembly of Multiamino Based Structures. Tetrahedron Lett 1998, 39, 3121-4.
【2】 Wald, S.A.; Hong, Y.; Wilkinson, H.S.; Senanayake, C.H.; Tanoury, G.J.; Bakale, R.P.; Palladium catalyzed amination of 2-chloro-1,3-azole derivatives: Mild entry to potent H1-antihistaminic norastemizole. Tetrahedron Lett 1997, 38, 5607-10.
【3】 Senanayake, C.; Hong, Y.; Bakale, R.; Handley, D.A.; Norastemizole. Drugs Fut 1998, 23, 9, 966.

中间体序号	中间体编号	品名	CAS号	分子式	供应商	用于合成
(I)	12043	1-(4-Fluorobenzyl-2-chlorobenzimidazol; 2-Chloro-1-(4-fluorobenzyl)-1H-benzimidazole; 1-(4-Fluorobenzyl)-2-chlorobenzimidazole	84946-20-3	C₁₄H₁₀ClFN₂	详情	详情
(II)	17502	4-piperidinylamine; 4-piperidinamine; 4-aminopiperidine	13035-19-3	C₅H₁₂N₂	详情	详情

Extended Information