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1. 发明授权

US08367824B2 Process for producing quinazolin-4-one derivative 失效
标题翻译：喹唑啉-4-酮衍生物的制备方法
公开(公告)号：US08367824B2
公开(公告)日：2013-02-05
申请号：US10502734
申请日：2003-01-28
申请人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Takashi Harada , Hiroyuki Oda
发明人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Takashi Harada , Hiroyuki Oda
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。

2. 发明申请

US20050130995A1 Process for producing 4-aminoquinazoline compound 审中-公开
标题翻译： 4-氨基喹唑啉化合物的制备方法
公开(公告)号：US20050130995A1
公开(公告)日：2005-06-16
申请号：US10503664
申请日：2003-02-06
申请人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Takashi Harada , Hiroyuki Oda
发明人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Takashi Harada , Hiroyuki Oda
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。

3. 发明申请

US20050080262A1 Process for producing quinazolin-4-one derivative 失效
标题翻译：喹唑啉-4-酮衍生物的制备方法
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。

4. 发明授权

US06841681B2 Process for producing quinoline carboxyaldehyde derivative and intermediate thereof 失效
标题翻译：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。

5. 发明授权

US08318932B2 Process for producing 4-aminoquinazoline compound 失效
标题翻译： 4-氨基喹唑啉化合物的制备方法
公开(公告)号：US08318932B2
公开(公告)日：2012-11-27
申请号：US12400895
申请日：2009-03-10
申请人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Takashi Harada , Hiroyuki Oda
发明人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Takashi Harada , Hiroyuki Oda
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）。

6. 发明授权

US07232903B2 Process for producing quinazolin-4-one and derivatives thereof 有权
标题翻译：喹唑啉-4-酮及其衍生物的制备方法
公开(公告)号：US07232903B2
公开(公告)日：2007-06-19
申请号：US10499361
申请日：2002-12-19
申请人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Takashi Harada , Hiroyuki Oda
发明人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Takashi Harada , Hiroyuki Oda
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。

7. 发明申请

US20050124809A1 Process for producing quinazolin-4-one and derivatives thereof 有权
标题翻译：喹唑啉-4-酮及其衍生物的制备方法
公开(公告)号：US20050124809A1
公开(公告)日：2005-06-09
申请号：US10499361
申请日：2002-12-19
申请人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Takashi Harada , Hiroyuki Oda
发明人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Takashi Harada , Hiroyuki Oda
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。

8. 发明授权

US07741497B2 Processes for preparing alkyl 3-(4-tetrahydropyranyl)-3-oxopropanoate compound and 4-acyltetrahydropyrane 失效
标题翻译：制备3-（4-四氢吡喃基）-3-氧代丙酸烷基酯化合物和4-酰基四氢吡喃的方法
公开(公告)号：US07741497B2
公开(公告)日：2010-06-22
申请号：US10583473
申请日：2004-12-17
申请人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Keiji Iwamoto , Takashi Harada
发明人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Keiji Iwamoto , Takashi Harada
IPC分类号： C07D309/06
CPC分类号： C07D309/06
摘要： The present invention is to provide a process for preparing an alkyl 3-(4-tetrahydropyranyl)-3-oxopropanoate compound represented by the formula (1): wherein R1 and R2 may be the same or different from each other, and represent a group which does not participate in the reaction, and R1 and R2 may be bonded to form a ring, and the ring may contain a hetero atom(s), and R3 represents a hydrocarbon group, which comprises reacting 4-acyltetrahydropyran represented by the formula (2): wherein R1 and R2 have the same meanings as defined above, and a carbonic acid diester represented by the formula (3): wherein R3 has the same meanings as defined above, and two R3s may be bonded to each other to form a ring, in the presence of a base, and a process for preparing 4-acyltetrahydropyran.
摘要翻译：本发明提供一种制备式（1）表示的3-（4-四氢吡喃基）-3-氧代丙酸烷基酯化合物的方法：其中R 1和R 2可以相同或不同，并且表示基团其不参与反应，并且R 1和R 2可以键合形成环，并且该环可以含有杂原子，并且R 3表示烃基，其包括使由式（Ⅳ）表示的4-酰基四氢吡喃与 2）：其中R1和R2具有与上述相同的含义，和由式（3）表示的碳酸二酯：其中R 3具有与上述相同的含义，并且两个R 3可以彼此键合形成在碱的存在下，以及制备4-酰基四氢吡喃的方法。

9. 发明授权

US07619084B2 Process for preparing 4-aminopyrimidine compound 失效
标题翻译： 4-氨基嘧啶化合物的制备方法
公开(公告)号：US07619084B2
公开(公告)日：2009-11-17
申请号：US11666510
申请日：2005-10-28
申请人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Takashi Harada
发明人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Takashi Harada
IPC分类号： C07D239/02
CPC分类号： C07D239/42
摘要： The present invention is to provide a process for preparing a 4-aminopyrimidine compound represented by the formula (3): wherein R1 and R2 each represent a hydrogen atom or group which does not participate in the reaction and which may have a substituent(s), and R1 and R2 may be bonded to each other to form a ring, and R4 represents a hydrogen atom or a hydrocarbon group, which comprises reacting ammonia, a 3-substituted or unsubstituted acrylonitrile compound represented by the formula (1): CR1(CN)═CR2Y (1) wherein R1 and R2 have the same meanings as defined above, and Y represents an amino group or OR, where R represents a hydrogen atom or a hydrocarbon group, and an organic acid compound represented by the formula (2): (R3O)3CR4 (2) wherein R3 represents a hydrocarbon group, and R4 has the same meaning as defined above.
摘要翻译：本发明提供一种制备式（3）表示的4-氨基嘧啶化合物的方法：其中R1和R2各自表示氢原子或不参与反应的基团，并且可以具有取代基， R 1和R 2可以彼此键合形成环，R 4表示氢原子或烃基，其包括使氨，3-取代或未取代的由式（1）表示的丙烯腈化合物：CR1（ CN）-CR2Y（1）其中R1和R2具有与上述相同的含义，Y表示氨基或OR，其中R表示氢原子或烃基，和由式（2）表示的有机酸化合物）：（R3O）3CR4（2）其中R3表示烃基，R4具有与上述相同的含义。

10. 发明申请

US20080045712A1 Process for Preparing 4-Aminopyrimidine Compound 失效
标题翻译： 4-氨基嘧啶化合物的制备方法
公开(公告)号：US20080045712A1
公开(公告)日：2008-02-21
申请号：US11666510
申请日：2005-10-28
申请人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Takashi Harada
发明人： Shigeyoshi Nishino , Kenji Hirotsu , Hidetaka Shima , Takashi Harada
IPC分类号： C07D239/42
CPC分类号： C07D239/42
摘要： The present invention is to provide a process for preparing a 4-aminopyrimidine compound represented by the formula (3): wherein R1 and R2 each represent a hydrogen atom or group which does not participate in the reaction and which may have a substituent(s), and R1 and R2 may be bonded to each other to form a ring, and R4 represents a hydrogen atom or a hydrocarbon group, which comprises reacting ammonia, a 3-substituted or unsubstituted acrylonitrile compound represented by the formula (1): CR1(CN)═CR2Y (1) wherein R1 and R2 have the same meanings as defined above, and Y represents an amino group or OR, where R represents a hydrogen atom or a hydrocarbon group, and an organic acid compound represented by the formula (2): (R3O)3CR4 (2) wherein R3 represents a hydrocarbon group, and R4 has the same meaning as defined above.
摘要翻译：本发明提供一种制备由式（3）表示的4-氨基嘧啶化合物的方法：其中R 1和R 2各自表示氢原子或基团其不参与反应并且可以具有取代基，R 1和R 2可以彼此键合形成环，并且R 其包括使氨，式（1）表示的3-取代或未取代的丙烯腈化合物：<？in-line-formula description =“In- 线公式“end =”lead“？> CR <1>（CN）-CR 2 Y（1）<？in-line-formula description =”在线公式 “其中R 1和R 2”具有与上述相同的含义，Y表示氨基或OR，其中R表示氢原子或烃基，以及由式（2）表示的有机酸化合物：<？in-line-formula description =“In-line Form （“O”）3“（4）”（2）<？in-line-formula description = 其中R 3表示烃基，并且R 4具有与上述相同的含义，“直链式”末端=“尾”→其中R 3表示烃基。

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