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公开(公告)号:EP4177244A2
公开(公告)日:2023-05-10
申请号:EP22198307.5
申请日:2020-07-10
申请人: Adama Agan Ltd.
发明人: Barda, Barda , Papo, Nitsan , Recsei, Carl
IPC分类号: C07D261/04 , C07C41/22 , C07C43/225 , C07D231/20 , C07D413/12
摘要: The invention relates to a process for preparing immediate precursors for pyroxasulfone and fenoxasulfone preparation of the formula (I). The process comprises a bromination reaction of a benzylic position without light irradiation (step a), followed by thoination reaction, which substitutes the bromine atom (step b) and after the protecting group is removed, and the revealed thiol or thiolate reacts with a substituted isoxazoline bearing a leaving group at the 3-position (step c).
wherein
Y = protecting group
In another variant of the invention the pyroxasulfone or fenoxasulfone immediate precursor is synthesized from the arylmethyl bromide by first forming a carbon-sulfur bond at the 3-position of a 2-isoxazoline through displacement of a leaving group at the 3-position (particularly acid derived residues such as phosphoryl, sulfanyl, halo, cyano or carboxyl groups) by an appropriate thionating reagent. The resulting adducts, which is a S-protected 3-thio-2-isoxazoline, may be treated with base to remove the protecting group, to reveal a thiol or thiolate which may subsequently react with the arylmethyl bromide to form the Pyroxasulfone or Fenoxasulfone immediate precursor.
Ar = aryl, Y = protecting group and X = leaving group-
公开(公告)号:EP3872055A1
公开(公告)日:2021-09-01
申请号:EP19876774.1
申请日:2019-10-23
发明人: ITO, Hajime , KUBOTA, Koji
IPC分类号: C07C1/32 , C07C15/14 , C07C15/24 , C07C19/08 , C07C41/22 , C07C43/205 , C07C45/68 , C07C69/76 , C07C209/10 , C07C209/68 , C07C211/48 , C07C211/54 , C07C211/58 , C07C211/61 , C07D333/08 , C07D333/36 , C07F5/02 , C09B47/00 , C07C17/275 , C07C49/784 , C07B61/00
摘要: Disclosed is a cross-coupling reaction method which forms a chemical bond selected from C-N, C-B, C-C, C-O and C-S bonds, the method comprising:
preparing an aromatic compound (1) having a leaving group;
preparing a compound (2) capable of undergoing a cross-coupling reaction selected from an aromatic amino compound (2-1), a diboronic acid ester or the like (2-2), an aromatic boronic acid or the like (2-3), an aromatic compound (2-4) having a hydroxyl group and an aromatic compound (2-5) having a thiol group; and
performing a cross-coupling reaction of the compound (1) with the compound (2) in the presence of a palladium catalyst, a base and a compound (4) having a carbon-carbon double bond or a carbon-carbon triple bond, in the absence of a solvent.-
公开(公告)号:EP3148693B1
公开(公告)日:2019-07-17
申请号:EP15799480.7
申请日:2015-04-23
IPC分类号: C07F15/00 , C07C5/03 , C08C19/02 , C08L15/00 , C07C29/17 , C07C67/303 , C07C41/22 , C07C201/12 , C07C45/63
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公开(公告)号:EP3042889B1
公开(公告)日:2019-02-27
申请号:EP14841616.7
申请日:2014-09-02
申请人: AGC Inc.
发明人: TAKAHIRA, Yusuke
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公开(公告)号:EP3299364A1
公开(公告)日:2018-03-28
申请号:EP15892188.2
申请日:2015-05-19
发明人: ZHENG, Zhiguo
IPC分类号: C07D311/58 , C07D303/22 , C07D301/14 , C07D301/19 , C07F7/08 , C07C41/22 , C07C43/225 , C07C41/18 , C07C41/30 , C07C43/23 , C07C41/20
CPC分类号: C07D311/76 , A61K31/353 , A61P9/08 , A61P9/12 , C07C41/18 , C07C41/20 , C07C41/22 , C07C41/30 , C07C43/225 , C07C43/23 , C07C43/295 , C07D301/14 , C07D301/19 , C07D303/22 , C07D303/36 , C07D311/58 , C07F7/08
摘要: The present invention relates to nebivolol synthesis method and intermediate compound thereof. Specifically, the present invention relates to a method for synthesizing nebivolol, intermediate compound thereof, and a method for preparing the intermediate compound.
摘要翻译: 本发明涉及奈比洛尔合成方法及其中间体化合物。 具体而言,本发明涉及合成奈必洛尔的方法,其中间体化合物以及制备该中间体化合物的方法。
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公开(公告)号:EP3284736A1
公开(公告)日:2018-02-21
申请号:EP17173035.1
申请日:2009-10-20
申请人: NUtech Ventures
发明人: Dimagno, Stephen
IPC分类号: C07C213/08 , C07C219/18 , C07D213/06 , C07C43/247 , C07D233/06 , C07D277/22 , C07C41/18 , C07C227/16 , C07C253/30 , C07C269/06 , C07C271/66 , C07C41/22
CPC分类号: C07D213/06 , C07B2200/05 , C07C41/18 , C07C41/22 , C07C227/16 , C07C253/30 , C07C269/06 , C07C271/66 , C07D233/06 , C07D277/22 , C07C229/36 , C07C255/50 , C07C43/225
摘要: This disclosure relates to reagents and methods useful in the synthesis of aryl fluorides, for example, in the preparation of 18 F labeled radiotracers. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.
摘要翻译: 本公开涉及可用于合成芳基氟化物的试剂和方法,例如制备18 F标记的放射性示踪剂。 本文提供的试剂和方法可以用于获得宽范围的化合物,包括芳族化合物,杂芳族化合物,氨基酸,核苷酸和合成化合物。
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公开(公告)号:EP3237367A1
公开(公告)日:2017-11-01
申请号:EP15874088.6
申请日:2015-12-04
CPC分类号: C07C43/126 , C07C17/087 , C07C17/093 , C07C17/208 , C07C19/16 , C07C21/18 , C07C41/18 , C07C41/20
摘要: Described herein is method of making a halogenated partially fluorinated compound, comprising: (a) providing a compound having the following structure of formula (I): Rf—CF═CXY wherein X and Y are independently selected from F and Cl; wherein Rf is a fluorinated monovalent group comprising 1 to 10 carbon atoms; (b) contacting the compound with at least one of (i) an iodine or bromine containing salt in the presence of an acid; and (ii) aqueous solution of HZ wherein Z is selected from I and Br to form the halogenated partially fluorinated compound of the formula (II): R′f—CFH—CXYZ wherein X and Y are independently selected from F and Cl; Z is selected from I and Br; and R′f is a fluorinated monovalent group comprising 1 to 10 carbon atoms.
摘要翻译: 本文描述了制备卤化部分氟化的化合物的方法,其包括:(a)提供具有以下式(I)结构的化合物:其中X和Y独立地选自F和C1; 其中R f是包含1至10个碳原子的氟化一价基团; (b)使所述化合物与(i)在酸存在下的含碘或含溴盐中的至少一种接触; 和(ii)HZ的水溶液,其中Z选自I和Br以形成式(II)的卤化的部分氟化的化合物:其中X和Y独立地选自F和C1; Z选自I和Br; 并且R'f是包含1至10个碳原子的氟化一价基团。
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8.
公开(公告)号:EP1886986B1
公开(公告)日:2017-06-21
申请号:EP06756422.9
申请日:2006-05-22
申请人: Unimatec Co., Ltd.
发明人: KOKIN, Keisuke, Unimatec Co., Ltd. , URATA, Kimihiko, Unimatec Co., Ltd. , SONOI, Takehiro, Unimatec Co., Ltd.
CPC分类号: C07C41/22 , C07C43/126
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公开(公告)号:EP2537826B1
公开(公告)日:2017-03-08
申请号:EP12185395.6
申请日:2009-10-20
申请人: NUtech Ventures
发明人: Dimagno, Stephen
IPC分类号: C07C213/08 , C07C219/18 , C07D213/06 , C07C43/247 , C07D233/06 , C07D277/22 , C07C41/18 , C07C43/225 , C07C227/16 , C07C253/30 , C07C269/06 , C07C271/66 , C07C41/22
CPC分类号: C07D213/06 , C07B2200/05 , C07C41/18 , C07C41/22 , C07C227/16 , C07C253/30 , C07C269/06 , C07C271/66 , C07D233/06 , C07D277/22 , C07C229/36 , C07C255/50 , C07C43/225
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10.
公开(公告)号:EP2593417B1
公开(公告)日:2017-02-01
申请号:EP11731309.8
申请日:2011-07-05
发明人: TORTELLI, Vito , GALIMBERTI, Marco
CPC分类号: C07C17/04 , C07C41/22 , C07C19/12 , C07C43/123
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