专利号:US-4383949-A 优先权日:1980-07-16 标题:Preparation of 3-bromo-4-fluorobenzaldehyde and its acetals 发明人:MAURER FRITZ; RIEBEL HANS-JOCHEM; PRIESNITZ UWE; KLAUKE ERICH 权利人:BAYER AG 摘要:A process for the preparation of a 3-bromo-4-fluorobenzaldehyde acetal of the formula ##STR1## in which R 1 is methyl or ethyl, n which comprises reacting a 3-bromo-4-fluoro-benzoic acid halide with ammonia to form 3-bromo-4-fluoro-benzoic acid amide, dehydrating said amide to form 3-bromo-4-fluoro-benzonitrile, reacting the nitrile with formic acid in the presence of a catalyst at a temperature between about 0° and 150° C. to form 3-bromo-4-fluorobenzaldehyde, and reacting said aldehyde with R 1 OH or a derivative thereof capable of forming an acetal. The amide and nitrile are new compounds. The acetals are known intermediates in the synthesis of pyrethroid-like insecticides.
专利号:US-4446075-A 优先权日:1980-02-22 标 题:Substituted bromofluorobenzene derivatives and process for its manufacture 发明人:EIGLMEIER KURT; KNIEPS REINHARD 权利人:RIEDEL DE HAEN AG 摘要:Substituted bromofluorobenzene, wherein the fluorine is in para-position and the bromine in meta-position to another substituent, is prepared by direct bromination of the corresponding fluorobenzene derivative. Bromination is advantageously carried out in the presence of a catalyst, preferably a metal or metal salt. The elementary bromine is used in an amount of 0.9 to 1.3 mols per mol of fluorobenzene derivative and the reaction temperature is between 20° and 200° C. The bromofluorobenzene derivatives are suitable for the synthesis of medicaments and plant protective agents.
专利号:WO-2023057548-A1 优先权日:2021-10-07 标题:Ccr6 receptor modulators 发明人:AISSAOUI HAMED; ALLEMANN OLIVER; CAROFF EVA; MEYER EMMANUEL; RICHARD-BILDSTEIN SYLVIA 权利人:IDORSIA PHARMACEUTICALS LTD 摘要:The present invention relates to compounds of Formula (I), their synthesis and use as CCR6 receptor modulators for the prevention or treatment of e.g. inflammatory/autoimmune diseases/disorders and cancer.
专利号:US-7737166-B2 优先权日:2005-08-17 标 题:Antifungal bicyclic hetero ring compounds 发明人:KAWAKAMI KATSUHIRO; KANAI KAZUO; HORIUCHI TAKAO; TAKESHITA HIROSHI; KOBAYASHI SYOZO; SUGIMOTO YUICHI; ACHIWA ISSEI; KUROYANAGI JUNICHI 权利人:DAIICHI SANKYO CO LTD 摘要:A 1,6-β-glucan synthetase inhibitor is provided, having potent growth inhibition and having excellent safety. A compound is provided, capable of expressing in a wide spectral range and specifically or selectively, an antifungal effect based on its functional mechanism of 1,6-β-glucan synthesis inhibition. Also provided is a drug, a salt or hydrate thereof, especially an antifungal that contains the compound. Concretely, provided is a compound of the following formula (I), its salt or hydrate, and a drug or antifungal containing, as the active ingredient, the compound, its salt or hydrate:
专利号:US-9198917-B2 优先权日:2012-12-11 标题:Hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds 发明人:BRODNEY MICHAEL AARON; BECK ELIZABETH MARY; BUTLER CHRISTOPHER RYAN; DAVOREN JENNIFER ELIZABETH; O'NEILL BRIAN THOMAS 权利人:PFIZER 摘要:The present invention provides compounds of Formula I, and the tautomers thereof, and the pharmaceutically acceptable salts of the compounds and tautomers, wherein the compounds have the structure n nwherein the variables R 1 , R 2 , R 3 , R 4 and x are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.