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【结 构 式】

【分子编号】19968

【品名】1-ethyl-3-piperidinamine; 1-ethyl-3-piperidinylamine

【CA登记号】

【 分 子 式 】C7H16N2

【 分 子 量 】128.21752

【元素组成】C 65.57% H 12.58% N 21.85%

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:(VI)

The cyclization of 2-amino-5-iodobenzoic acid (I) with an excess of refluxing trifluoroacetic anhydride (II) by means of triethylamine gives 6-iodo-2-(trifluoromethyl)-3,1-benzoxazin-4-one (III), which is treated with conc. aqueous NH4OH to afford 6-iodo-2-(trifluoromethyl)quinazolin-4(3H)-one (IV). The reaction of (IV) with refluxing POCl3 yields 4-chloro-6-iodo-2-(trifluoromethyl)quinazoline (V), which is finally condensed with 1-Ethylpiperidine-3-amine (VI) by means of triethylamine in ether.

1 Ahn, K.; Cheng, X.-M.; Doherty, A.M.; Elslager, E.F.; Kornberg, B.; Lee, C.; Leonard, D.; Nikam, S.S.; Werbel, L.M. (Pfizer Inc.); Quinazolines as inhibitors of endothelin converting enzyme. EP 0799221; JP 1998510834; US 5658902; WO 9619474 .
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) 19964 5-Iodoanthranilic acid; 2-amino-5-iodobenzoic acid 5326-47-6 C7H6INO2 详情 详情
(III) 19965 6-iodo-2-(trifluoromethyl)-4H-3,1-benzoxazin-4-one C9H3F3INO2 详情 详情
(IV) 19966 6-iodo-2-(trifluoromethyl)-4(3H)-quinazolinone C9H4F3IN2O 详情 详情
(V) 19967 4-chloro-6-iodo-2-(trifluoromethyl)quinazoline C9H3ClF3IN2 详情 详情
(VI) 19968 1-ethyl-3-piperidinamine; 1-ethyl-3-piperidinylamine C7H16N2 详情 详情
Extended Information