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【结 构 式】

【分子编号】19570

【品名】4-bromo-1-(chloromethyl)-2-fluorobenzene

【CA登记号】

【 分 子 式 】C7H5BrClF

【 分 子 量 】223.4718032

【元素组成】C 37.62% H 2.26% Br 35.76% Cl 15.86% F 8.5%

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:(XIII)

3) The alkylation of 2-amino-4-chlorobenzamide (X) with ethyl bromoacetate (VI) by means of K2CO3 in hot DMF gives ethyl 2-(2-carbamoyl-4-chlorophenylamino)acetate (XI), which is cyclized with CDI at 150 C yielding ethyl 7-chloro-2,4-dioxo-1,2,3,4-tetrahydroquinazoline-1-acetate (XII). Finally, this compound is alkylated with 4-bromo-2-fluorobenzyl chloride (XIII) by means of NaH in DMF to afford quinazoline (VII) already obtained.

1 Hashimoto, M.; Oku, T.; Ito, Y.; Namiki, T.; Sawada, K.; Kasahara, C.; Baba, Y. (Fujisawa Pharmaceutical Co., Ltd.); New quinazoline derivs., process for their production and pharmaceutical compsns. comprising them. EP 0218999; JP 1987096476; JP 1989125322; JP 1989131164; US 4734419; US 4883800 .
2 Prous, J.; Castaner, J.; FR-74366. Drugs Fut 1989, 14, 1, 26.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(VI) 16640 Ethyl 2-bromoacetate; Ethyl bromoacetate 105-36-2 C4H7BrO2 详情 详情
(VII) 19564 ethyl 2-[3-(4-bromo-2-fluorobenzyl)-7-chloro-2,4-dioxo-3,4-dihydro-1(2H)-quinazolinyl]acetate C19H15BrClFN2O4 详情 详情
(X) 19567 2-amino-4-chlorobenzamide C7H7ClN2O 详情 详情
(XI) 19568 ethyl 2-[2-(aminocarbonyl)-5-chloroanilino]acetate C11H13ClN2O3 详情 详情
(XII) 19569 ethyl 2-[7-chloro-2,4-dioxo-3,4-dihydro-1(2H)-quinazolinyl]acetate C12H11ClN2O4 详情 详情
(XIII) 19570 4-bromo-1-(chloromethyl)-2-fluorobenzene C7H5BrClF 详情 详情
Extended Information