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1.发明授权Process for producing quinoline carboxyaldehyde derivative and intermediate thereof 失效制备喹啉羧醛衍生物及其中间体的方法公开(公告)号：US06841681B2
公开(公告)日：2005-01-11
申请号：US10468062
申请日：2002-02-14
申请人： Katsumasa Harada , Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Naoko Okada , Takashi Harada , Akira Nakamura , Hiroyuki Oda
发明人： Katsumasa Harada , Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Naoko Okada , Takashi Harada , Akira Nakamura , Hiroyuki Oda
IPC分类号： C07D215/14 , C07D215/54 , C07C225/22 , C07C255/17 , C07D215/12
CPC分类号： C07D215/14
摘要： 2-Cyclopropyl-4-(4′-fluorophenyl)quinoline-3-carboxyaldehyde useful as a material for pharmaceutical products, can be obtained by reacting 3-cyclopropyl-3-oxopropanenitrile with 2-amino-4′-fluorobenzophenone to obtain 2-cyclopropyl-4-(4′-fluorophenyl)quinoline-3-carbonitrile, and reducing it.
摘要翻译： 可用作药物物质的2-环丙基-4-（4'-氟苯基）喹啉-3-甲醛可以通过3-环丙基-3-氧代丙腈与2-氨基-4'-氟二苯甲酮反应得到2- 环丙基-4-（4'-氟苯基）喹啉-3-腈，并还原。
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公开(公告)号：US06541636B2
公开(公告)日：2003-04-01
申请号：US10181973
申请日：2002-07-24
IPC分类号： C07D21504
CPC分类号： C07D215/12
摘要： 3-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]prop-2-enenitrile is prepared by reacting 2-cyclopropyl-4-(4-fluorophenyl)quinoline-3-carbaldehyde with acetonitrile in the presence of a base and then adding a dehydrating to the reaction mixture to conduct dehydration. Under ordinary conditions, novel 3-[2-cyclopropyl-4-(4-fluoro-phenyl)-quinolin-3-yl]-3-hydroxypropionitrile is formed as an intermediate in the above reaction. Incidentally, when the above reaction is conducted in an organic solvent, 3-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-prop-2-enenitrile is directly formed.
摘要翻译： 3- [2-环丙基-4-（4-氟苯基）-3-喹啉基]丙-2-烯腈是通过2-环丙基-4-（4-氟苯基）喹啉-3-甲醛与乙腈在 然后向反应混合物中加入脱水剂进行脱水。 在常规条件下，在上述反应中形成新的3- [2-环丙基-4-（4-氟 - 苯基） - 喹啉-3-基] -3-羟基丙腈作为中间体。 顺便提及，当上述反应在有机溶剂中进行时，直接形成3- [2-环丙基-4-（4-氟苯基）-3-喹啉基] - 丙-2-烯腈。
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公开(公告)号：US08367824B2
公开(公告)日：2013-02-05
申请号：US10502734
申请日：2003-01-28
IPC分类号： C07D239/72
CPC分类号： C07D239/88 , C07C67/31 , C07C69/92 , C07C201/08 , C07C205/59 , C07C205/60 , C07C227/04 , C07C229/56 , C07C229/64 , C07D239/90
摘要： A process for producing a quinazolin-4-one compound having the formula: [wherein R1, R2, R3 and R4 each represents a group not participating in the below-mentioned reaction, and R1, R2, R3 and R4 can be combined together to form a ring] which comprises reacting an anthranilic acid derivative having the formula: [wherein R5 is a hydrogen atom or a hydrocarbyl group] with a formic acid derivative in the presence of an ammonium carboxylate.
摘要翻译： 制备具有下式的喹唑啉-4-酮化合物的方法：其中R 1，R 2，R 3和R 4各自表示不参与下述反应的基团，R 1，R 2，R 3和R 4可以组合在一起至 形成环]，其包括在羧酸铵存在下使具有式[其中R5是氢原子或烃基]的邻氨基苯甲酸衍生物与甲酸衍生物反应。
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公开(公告)号：US20050130995A1
公开(公告)日：2005-06-16
申请号：US10503664
申请日：2003-02-06
IPC分类号： C07D239/88 , C07D239/94 , A61K31/517
CPC分类号： C07D239/88 , C07D239/94
摘要： A 4-aminoquinazoline derivative can be obtained by the steps of reacting quinazolin-4-one or its derivative with a chlorinating agent in a first organic solvent in the presence of an organic base, and subsequently reacting the reaction product with an amine compound represented by the formula R5—NH—R6 (each of R5 and R6 represents hydrogen or an optionally substituted hydrocarbyl group) in the presence of a second organic solvent.
摘要翻译： 4-氨基喹唑啉衍生物可以通过以下步骤获得：将喹唑啉-4-酮或其衍生物与氯化剂在有机碱存在下在第一有机溶剂中反应，然后使反应产物与由 式R 5 -NH-R 6（R 5和R 6各自表示氢或任选地 取代的烃基）在第二有机溶剂的存在下进行。
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公开(公告)号：US20050080262A1
公开(公告)日：2005-04-14
申请号：US10502734
申请日：2003-01-28
申请人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Takashi Harada , Hiroyuki Oda , Takeshi Takahashi , Shinobu Suzuki
发明人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Takashi Harada , Hiroyuki Oda , Takeshi Takahashi , Shinobu Suzuki
IPC分类号： C07C201/08 , C07C205/59 , C07C205/60 , C07C227/04 , C07C229/56 , C07C229/64 , C07D239/88 , C07D239/90 , C07D239/72
CPC分类号： C07D239/88 , C07C67/31 , C07C69/92 , C07C201/08 , C07C205/59 , C07C205/60 , C07C227/04 , C07C229/56 , C07C229/64 , C07D239/90
摘要： A process for producing a quinazolin-4-one compound having the formula: [wherein R1, R2, R3 and R4 each represents a group not participating in the below-mentioned reaction, and R1, R2, R3 and R4 can be combined together to form a ring] which comprises reacting an anthranilic acid derivative having the formula: [wherein R5 is a hydrogen atom or a hydrocarbyl group] with a formic acid derivative in the presence of an ammonium carboxylate.
摘要翻译： 制备具有下式的喹唑啉-4-酮化合物的方法：其中R 1，R 2，R 3和R 4各自表示不参与下述反应的基团，和 R 1，R 2，R 3和R 4可以组合在一起形成环]，其包括使具有下式的邻氨基苯甲酸衍生物：其中R 5是氢原子或 烃基]与甲酸衍生物在羧酸铵存在下反应。
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公开(公告)号：US08318932B2
公开(公告)日：2012-11-27
申请号：US12400895
申请日：2009-03-10
IPC分类号： C07D239/72
CPC分类号： C07D239/88 , C07D239/94
摘要： A 4-aminoquinazoline derivative can be obtained by the steps of reacting quinazolin-4-one or its derivative with a chlorinating agent in a first organic solvent in the presence of an organic base, and subsequently reacting the reaction product with an amine compound represented by the formula R5—NH—R6 (each of R5 and R6 represents hydrogen or an optionally substituted hydrocarbyl group) in the presence of a second organic solvent.
摘要翻译： 4-氨基喹唑啉衍生物可以通过以下步骤获得：将喹唑啉-4-酮或其衍生物与氯化剂在有机碱存在下在第一有机溶剂中反应，然后使反应产物与由 在第二有机溶剂的存在下，式R5-NH-R6（R5和R6各自表示氢或任选取代的烃基）。
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公开(公告)号：US07232903B2
公开(公告)日：2007-06-19
申请号：US10499361
申请日：2002-12-19
IPC分类号： C07D239/88
CPC分类号： C07D239/88 , C07C229/56
摘要： A process for preparing quinazolin-4-one or its derivative by reacting anthranilic acid or its derivative with formic acid or its derivative in the presence of ammonia, or by reacting ammonium anthranilate or its derivative with formic acid or its derivative.
摘要翻译： 通过邻氨基苯甲酸或其衍生物与甲酸或其衍生物在氨的存在下反应制备喹唑啉-4-酮或其衍生物的方法，或通过使邻氨基苯甲酸铵或其衍生物与甲酸或其衍生物反应。
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公开(公告)号：US20050124809A1
公开(公告)日：2005-06-09
申请号：US10499361
申请日：2002-12-19
IPC分类号： C07C229/56 , C07D239/88
CPC分类号： C07D239/88 , C07C229/56
摘要： A process for preparing quinazolin-4-one or its derivative by reacting anthranilic acid or its derivative with formic acid or its derivative in the presence of ammonia, or by reacting ammonium anthranilate or its derivative with formic acid or its derivative.
摘要翻译： 通过邻氨基苯甲酸或其衍生物与甲酸或其衍生物在氨的存在下反应制备喹唑啉-4-酮或其衍生物的方法，或通过使邻氨基苯甲酸铵或其衍生物与甲酸或其衍生物反应。
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公开(公告)号：US07049458B2
公开(公告)日：2006-05-23
申请号：US10451280
申请日：2001-12-25
IPC分类号： C07C255/03
CPC分类号： C07C253/30 , C07C2601/02 , C07C255/17 , C07C255/31
摘要： A process comprising reacting an aliphatic carboxylic ester compound with acetonitrile in the presence of a metal alkoxide to yield a metal salt of a β-ketonitrile compound, subsequently transferring the salt to an aqueous medium, and neutralizing the solution to obtain the β-ketonitrile compound in a free state, wherein a water-immisible organic solvent and water are added to the reaction mixture containing the β-ketonitrile compound metal salt yielded to transfer the metal salt to the water, the resultant aqueous solution of the β-ketonitrile compound metal salt is separated from the organic solvent by phase separation or another technique and then neutralized, and the resultant free β-ketonitrile compound is taken out by extraction with an organic solvent.
摘要翻译： 一种方法，其包括在金属醇盐存在下使脂族羧酸酯化合物与乙腈反应，得到β-酮腈化合物的金属盐，随后将盐转移到水性介质中，并中和溶液以获得β-酮腈化合物 在游离状态下，其中将水不溶性有机溶剂和水加入到含有将金属盐转移到水中的β-酮腈复合金属盐的反应混合物中，得到β-酮腈复合金属盐水溶液 通过相分离或其它技术与有机溶剂分离，然后中和，所得游离β-酮腈化合物通过用有机溶剂萃取而取出。
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10.发明授权Processes for producing tetrahydropyranyl-4-sulfonates and 4-aminotetrahydropyran compounds 失效制备四氢吡喃-4-磺酸盐和4-氨基四氢吡喃化合物的方法公开(公告)号：US06653489B2
公开(公告)日：2003-11-25
申请号：US10148750
申请日：2002-06-03
IPC分类号： C07D30902
CPC分类号： C07D309/14 , C07D309/08
摘要： The present invention is to provide a process for producing a tetrahydropyranyl-4-sulfonate which comprises allowing 3-buten-1-ol which is easily available to react with a formaldehyde compound and an organic sulfonic acid, and a process for producing a 4-aminotetrahydropyrane derivative, which is industrially useful, under mild conditions and by a simple and easy method to produce the 4-aminotetrahydropyrane derivative in high yield.
摘要翻译： 本发明提供一种四氢吡喃基-4-磺酸盐的制备方法，其包括使容易获得的3-丁烯-1-醇与甲醛化合物和有机磺酸反应，以及制备4- 氨基四氢吡喃衍生物，其在工业上可用，在温和条件下，通过简单和容易的方法以高产率生产4-氨基四氢吡喃衍生物。
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