CAS: 1082040-43-4; Methyl 6-Fluoro-1H-Indole-4-Carboxylate

相似化合物

885518-27-4 649550-97-0 1220039-52-0

5-氟-2-甲基苯甲酸甲酯置于氢气,乙酸酐,溶剂黄146,Potassium Nitrate,三乙胺体系中,用 甲醇 用作溶剂,10.0~100.0 °C,1.01 Mpa 条件下,反应 28.0H,反应生成6-氟-1H-吲唑-4-甲酸甲酯
参考文献:抗卵巢癌药物rucaparib关键中间体的制备方法
标题:抗卵巢癌药物rucaparib关键中间体的制备方法
摘要:抗卵巢癌药物rucaparib关键中间体的制备方法,涉及医药中间体的制备.化合物1以甲醇和环己烷用作溶剂,以对甲苯磺酸为催化剂,反应后得化合物2;以醋酸和醋酸酐用作溶剂,将化合物2与硝酸钾反应,得化合物3;化合物3以n,N‑二甲基甲酰胺二甲基缩醛用作溶剂,三乙胺为催化剂,反应,得化合物4;化合物4以甲醇用作溶剂,雷尼镍为催化剂,反应,得化合物5,即抗卵巢癌药物rucaparib关键中间体:6‑氟‑1H‑吲唑‑4‑甲酸甲酯.避免硝硫混酸硝化反应和废水废气排放,安全环保.原料易得价格低,提高反应收率,便于工业化生产.

专利信息

专利号:WO-2019020508-A1
优先权日:2017-07-26
标 题 :PROCESS FOR THE PREPARATION OF HIGH-PURITY RUCAPARIB
发明人：BELOGI GIANLUCA; MAZZONI ANDREA; SERRA STEFANO; NOVO BARBARA
权利人:OLON SPA
摘要:The present invention relates to a new low environmental impact method for the synthesis of rucaparib with high yield and purity, said process comprising a regioselective coupling reaction between indole and iodo-aryl, carried out in water in the presence of a catalyst. The process of the invention is industrially advantageous because in the key coupling step, high regioselectivity is achieved without the use of complex intermediates or potentially toxic and environmentally harmful solvents.