CAS: 162401-62-9; 3-(Cyclopropylmethoxy)-4-(Difluoromethoxy)Benzoic Acid

上下游产品

3-(Cyclopropylmethoxy)-4-(Difluoromethoxy)-Benzoic Acid Methyl Ester
4-(二氟甲氧基)-3-(环丙基甲氧基)苯甲醛 3-(Cyclopropylmethoxy)-4-(Difluoromethoxy)Benzaldehyde 151103-09-2
罗氟司特杂质d 3-(Cyclopropylmethoxy)-4-Hydroxybenzoic Acid 1243391-44-7
3-(环丙基甲氧基)-4-羟基苯甲酸甲酯 Methyl 3-(Cyclopropylmethoxy)-4-Hydroxybenzoate 848574-60-7
3-环丙基甲氧基-4-羟基苯甲醛 3-(Cyclopropylmethoxy)-4-Hydroxybenzaldehyde 25934-52-5
4-二氟甲氧基-3-甲氧基苯甲醛 4-(Difluoromethoxy)-3-Methoxybenzaldehyde 162401-70-9
4-二氟甲氧基-3-羟基苯甲醛 4-Difluoromethoxy-3-Hydroxybenzaldehyde 151103-08-1
4-Bromo-2-(Cyclopropylmethoxy)-1-(Difluoromethoxy)Benzene 680184-55-8

3-羟基-4-碘苯甲酸甲酯置于copper(L) Iodide,8-羟基喹啉,氯化亚砜,Potassium Carbonate,Potassium Hydroxide,Sodium Hydroxide体系中,用 甲醇,二甲基亚砜,N,N-二甲基甲酰胺 用作溶剂,化学反应 39.25H,反应生成3-环丙甲氧基-4-二氟甲氧基苯甲酸
参考文献:通过铜催化的羟基化反应制备鲁氟司特的新途径
标题:通过铜催化的羟基化反应制备鲁氟司特的新途径
摘要:摘要 描述了一种向roflumilast的新途径,一种选择性的4型磷酸二酯酶(pde 4)抑制剂.合成过程从4-羟基-3-碘苯甲酸开始,通过铜催化的羟基化反应进入关键中间体3-(环丙基甲氧基)-4-(二氟甲氧基)苯甲酸,并利用酰胺偶联完成罗氟司特的总合成量80%让. 描述了一种向roflumilast的新途径,一种选择性的4型磷酸二酯酶(pde 4)抑制剂.合成过程从4-羟基-3-碘苯甲酸开始,通过铜催化的羟基化反应进入关键中间体3-(环丙基甲氧基)-4-(二氟甲氧基)苯甲酸,并利用酰胺偶联完成罗氟司特的总合成量80%让.
Doi:10.1055/s-0032-1317527

专利信息

专利号:US-9233925-B2
优先权日:2012-03-07
标 题:Process for preparation of roflumilast
发明人：CHEN YI-JING; PIKUL STANISLAW; KUO SHEN-CHUN; CHU GUO-DONG
权利人:SCINOPHARM CHANGSHU PHARMACEUTICALS LTD
摘要:The present invention provides novel processes for the preparation of N-substituted benzamides having the formula VIc: n nIn some embodiments, the invention provides a process for preparation of roflumilast and other pharmaceutically active species. Novel compounds, including intermediates for the synthesis of roflumilast, are also provided.

专利号:CN-102093194-A
优先权日:2010-12-24
标题 :A new method for the synthesis of 3-cyclopropylmethoxy-4-difluoromethoxybenzoic acid

专利号:US-9321726-B2
优先权日:2012-10-17
标题:Process for preparing roflumilast
发明人：SALAET FERRE JOSEP; MARQUILLAS OLONDRIZ FRANCISCO
权利人:INTERQUIM SA
摘要:The invention relates to a process for the preparation of Roflumilast by reaction of an activated form of 3-(cyclopropylmethoxy)-4-(difluoromethoxy)-benzoic acid with an activating agent selected from (a) carbonyldiimidazole (CDI), (b) 1,1′-carbonyl-di-(1,2,4-triazol) (CDT), (c) 1,1′-carbonyl-bis-(2-methylimidazol), (d), 1′-carbonyl-dipyperidin, (e) N,N′-dicyclohexylcarbodiimide (DCC), (f) N,N′-diisopropylcarbodiimide (DIC), (g) 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC) and a combination of one of the previous (a)-(g) with (h) N-hydroxysuccinimide or (i) N-hydroxyphthalimide, and the subsequent reaction with 3,5-dichloropyridine-4-amine in the presence of an inorganic base. The invention also relates to the synthesis intermediates.

专利号:CN-116803986-A
优先权日:2023-06-27
标 题:A kind of synthesis method of roxadustat intermediate

专利号:CN-119371301-A
优先权日:2023-07-27
标题:Roflumilast middle Synthesis process of intermediate

专利号:CN-116803986-B
优先权日:2023-06-27
标题:Synthesis method of roflumilast intermediate