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【结 构 式】

【分子编号】43690

【品名】7-ethyloctahydro-2H-pyrido[1,2-a]pyrazine

【CA登记号】

【 分 子 式 】C10H20N2

【 分 子 量 】168.28228

【元素组成】C 71.37% H 11.98% N 16.65%

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:(IV)

The cyclization of 5-ethylpiperidine-2-carboxylic acid ethyl ester (I) with aziridine (II) in ethanol gives 7-ethylperhydropyrido[1,2-a]pyrazin-1-one (III), which is reduced with LiAlH4 to yield 7-ethylperhydropyrido[1,2-a]pyrazine (IV). The reaction of (IV) with NaNO2/HCl, followed by reduction with LiAlH4, affords 7-ethylperhydropyrido[1,2-a]pyrazin-2-amine (V), which is finally condensed with rifamicin SV-3-carbaldehyde (VI).

1 Hauffe, S.; Tosch, W.; Batt, E.; Ashtekar, D.R.; Costa-Pereira, R.; Vischer, W.; Traxler, P.; Degen, P.; Zak, O.; Imhof, P.; Gowrishankar, R.; 3-Formylrifamycin SV-hydrazones with diazabicycloalkyl side-chains: New rifamycins aganist tuberculosis with long plasma half-lives. 27th Intersci Conf Antimicrob Agents Chemother 1987, Abst 278.
2 Traxler, P. (Novartis Corp.); Novel polycyclic hydrazones of rifamycins, their manufacture, and their pharmaceutical compsns. for treating tuberculosis. US 4681938 .
3 Traxler, P.; Vischer, W.; Zak, O.; New Rifamycins. Drugs Fut 1988, 13, 9, 845.
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) 43688 ethyl 5-ethyl-2-piperidinecarboxylate C10H19NO2 详情 详情
(II) 10151 Ethyleneimine; Aziridine; Azirane 151-56-4 C2H5N 详情 详情
(III) 43689 7-ethylhexahydro-2H-pyrido[1,2-a]pyrazin-1(6H)-one C10H18N2O 详情 详情
(IV) 43690 7-ethyloctahydro-2H-pyrido[1,2-a]pyrazine C10H20N2 详情 详情
(V) 43691 7-ethyloctahydro-2H-pyrido[1,2-a]pyrazin-2-amine; 7-ethyloctahydro-2H-pyrido[1,2-a]pyrazin-2-ylamine C10H21N3 详情 详情
(VI) 43692 26-formyl-2,15,17,27,29-pentahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-6,23-dioxo-8,30-dioxa-24-azatetracyclo[23.3.1.1(4,7).0(5,28)]triaconta-1(28),1(29),2,4,9,19,21,25,27-nonaen-13-yl acetate C38H47NO13 详情 详情
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