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【结 构 式】

【分子编号】51625

【品名】2-trifluoromethoxyaniline; alpha,alpha,alpha-trifluoro-o-anisidine; o-trifluoromethoxyaniline

【CA登记号】1535-75-7

【 分 子 式 】C7H6F3NO

【 分 子 量 】177.1259896

【元素组成】C 47.47% H 3.41% F 32.18% N 7.91% O 9.03%

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)

Diethyl malonate (I) was alkylated with 2-bromoethyl ethyl ether (II) to provide diethyl (2-ethoxyethyl)malonate (III). Subsequent condensation of malonate (III) with 2-(trifluoromethoxy)aniline (IV) in boiling diphenyl ether generated the furoquinoline derivative (V). This was then condensed with 2-methyl-4-methoxyaniline (VI) in refluxing diethylene glycol to furnish adduct (VII). Chlorination of pyrroloquinolone (VII) with phosphoryl chloride gave rise to the chloro pyrroloquinoline (VIII). The chloro group of (VIII) was finally displaced with ethanolamine (IX) at 190 C, yielding the title compound.

1 Kim, H.-J.; Kim, S.-S.; Yoo, Y.-K.; Kang, S.-K.; Cheon, H.-G.; Choi, J.-K.; Yum, E.-K. (Korea Research Institute of Chemical Technology); Pyrrolo[3,2-c]quinoline derivs. containing haloalkoxy group and pharmaceutically acceptable salts thereof. CA 2268166; EP 0966466; JP 2000504352; US 6011044; WO 9909029 .
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) 16829 Diethyl malonate 105-53-3 C7H12O4 详情 详情
(II) 34659 2-bromoethyl ethyl ether; 1-bromo-2-ethoxyethane 592-55-2 C4H9BrO 详情 详情
(III) 34660 diethyl 2-(2-ethoxyethyl)malonate C11H20O5 详情 详情
(IV) 51625 2-trifluoromethoxyaniline; alpha,alpha,alpha-trifluoro-o-anisidine; o-trifluoromethoxyaniline 1535-75-7 C7H6F3NO 详情 详情
(V) 51626 6-(trifluoromethoxy)-3,5-dihydrofuro[3,2-c]quinolin-4(2H)-one C12H8F3NO3 详情 详情
(VI) 40006 4-methoxy-2-methylphenylamine; 4-methoxy-2-methylaniline 102-50-1 C8H11NO 详情 详情
(VII) 51627 1-(4-methoxy-2-methylphenyl)-6-(trifluoromethoxy)-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-c]quinolin-4-one C20H17F3N2O3 详情 详情
(VIII) 51628 4-chloro-1-(4-methoxy-2-methylphenyl)-6-(trifluoromethoxy)-2,3-dihydro-1H-pyrrolo[3,2-c]quinoline; 4-chloro-1-(4-methoxy-2-methylphenyl)-2,3-dihydro-1H-pyrrolo[3,2-c]quinolin-6-yl trifluoromethyl ether C20H16ClF3N2O2 详情 详情
(IX) 10259 Ethanol amine;Ethanolamine;2-Aminoethanol; 2-Amino-1-ethanol;2-Aminoethyl alcohol 141-43-5 C2H7NO 详情 详情
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