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【结 构 式】

【分子编号】13027

【品名】4-(1-Piperidinylmethyl)-2-pyridinyl (Z)-4-(tetrahydro-2H-pyran-2-yloxy)-2-butenyl ether; 4-(1-Piperidinylmethyl)-2-[[(Z)-4-(tetrahydro-2H-pyran-2-yloxy)-2-butenyl]oxy]pyridine

【CA登记号】

【 分 子 式 】C20H30N2O3

【 分 子 量 】346.46988

【元素组成】C 69.33% H 8.73% N 8.09% O 13.85%

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:(VII)

The condensation of 2-chloro-4-(piperidin-1-ylmethyl)pyridine (V) with 4-(tetrahydropyranyloxy)-2(Z)-buten-1-ol (VI) by means of NaH in THF gives 4-(piperidin-1-ylmethyl)-2-[4-(tetrahydropyranyloxy)-2(Z)-butenyloxy)pyridine (VII), which is deprotected with 4-methylbenzenesulfonic acid in methanol, yielding the free butenol (VIII). The acylation of (VIII) with methanesulfonyl chloride in toluene affords the corresponding mesylate (IX), which is finally condensed with 2-(2-furylmethylsulfonyl)acetamide (X) (obtained from the corresponding 4-nitrophenyl ester (XI) with ammonia) by means of potassium tert-butoxide in toluene.

1 Iwata, H.; Matsumoto, H.; Matsumoto, M.; Sekine, Y.; Nishimura, M.; Hosoda, A. (UCB Japan); Methods of producing amino butene derivs. EP 0582304; JP 1994192195 .
2 Graul, A.; Prous, J.; Castaner, J.; Lafutidine. Drugs Fut 1994, 19, 9, 835.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(V) 13025 2-Chloro-4-(1-piperidinylmethyl)pyridine C11H15ClN2 详情 详情
(VI) 13026 (Z)-4-(Tetrahydro-2H-pyran-2-yloxy)-2-buten-1-ol C9H16O3 详情 详情
(VII) 13027 4-(1-Piperidinylmethyl)-2-pyridinyl (Z)-4-(tetrahydro-2H-pyran-2-yloxy)-2-butenyl ether; 4-(1-Piperidinylmethyl)-2-[[(Z)-4-(tetrahydro-2H-pyran-2-yloxy)-2-butenyl]oxy]pyridine C20H30N2O3 详情 详情
(VIII) 13028 (Z)-4-[[4-(1-Piperidinylmethyl)-2-pyridinyl]oxy]-2-buten-1-ol C15H22N2O2 详情 详情
(IX) 13029 (Z)-4-[[4-(1-piperidinylmethyl)-2-pyridinyl]oxy]-2-butenyl methanesulfonate C16H24N2O4S 详情 详情
(X) 13030 2-[(2-Furylmethyl)sulfinyl]acetamide C7H9NO3S 详情 详情
(XI) 13031 4-nitrophenyl 2-[(2-furylmethyl)sulfinyl]acetate C13H11NO6S 详情 详情
Extended Information