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1. 发明授权

US07816528B2 Preparation of aminopyrimidine compounds 有权
标题翻译：氨基嘧啶化合物的制备
公开(公告)号：US07816528B2
公开(公告)日：2010-10-19
申请号：US11933626
申请日：2007-11-01
申请人： Akio Matsushita , Mizuho Oda , Yasuhiro Kawachi , Jun-ichi Chika
发明人： Akio Matsushita , Mizuho Oda , Yasuhiro Kawachi , Jun-ichi Chika
IPC分类号： C07D239/34 , C07D239/22 , C07D239/42 , A61K31/505 , A61P3/06
CPC分类号： C07D239/22 , C07D239/30 , C07D239/34 , C07D239/36 , C07D239/42
摘要： A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.
摘要翻译：通过以下步骤制备式（3）的2-（N-甲基-N-甲磺酰基氨基）嘧啶化合物：[R是烃基]：（I）使异丁酰乙酸酯与4-氟苯甲醛和尿素反应质子化合物和金属盐的存在; （II）氧化步骤（I）的反应产物; （III）使步骤（II）的氧化产物与有机磺酰卤或有机磺酰酐反应; 和（IV）使步骤（III）的反应产物与N-甲基-N-甲磺酰胺反应。

2. 发明授权

US08614320B2 Preparation of aminopyrimidine compounds 有权
标题翻译：氨基嘧啶化合物的制备
公开(公告)号：US08614320B2
公开(公告)日：2013-12-24
申请号：US13523534
申请日：2012-06-14
申请人： Akio Matsushita , Mizuho Oda , Yasuhiro Kawachi , Jun-ichi Chika
发明人： Akio Matsushita , Mizuho Oda , Yasuhiro Kawachi , Jun-ichi Chika
IPC分类号： C07D239/36 , C07D239/42 , C07D239/22 , A61K31/505 , A61P3/06
CPC分类号： C07D239/22 , C07D239/30 , C07D239/34 , C07D239/36 , C07D239/42
摘要： A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.
摘要翻译：通过以下步骤制备式（3）的2-（N-甲基-N-甲磺酰基氨基）嘧啶化合物：[R是烃基]：（I）使异丁酰乙酸酯与4-氟苯甲醛和尿素反应质子化合物和金属盐的存在; （II）氧化步骤（I）的反应产物; （III）使步骤（II）的氧化产物与有机磺酰卤或有机磺酰酐反应; 和（IV）使步骤（III）的反应产物与N-甲基-N-甲烷磺酰胺反应。

3. 发明授权

US08222412B2 Preparation of aminopyrimidine compounds 有权
标题翻译：氨基嘧啶化合物的制备
公开(公告)号：US08222412B2
公开(公告)日：2012-07-17
申请号：US12889186
申请日：2010-09-23
申请人： Akio Matsushita , Mizuho Oda , Yasuhiro Kawachi , Jun-ichi Chika
发明人： Akio Matsushita , Mizuho Oda , Yasuhiro Kawachi , Jun-ichi Chika
IPC分类号： C07D239/34 , C07D239/22 , C07D239/42
CPC分类号： C07D239/22 , C07D239/30 , C07D239/34 , C07D239/36 , C07D239/42
摘要： A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.
摘要翻译：通过以下步骤制备式（3）的2-（N-甲基-N-甲磺酰基氨基）嘧啶化合物：[R是烃基]：（I）使异丁酰乙酸酯与4-氟苯甲醛和尿素反应质子化合物和金属盐的存在; （II）氧化步骤（I）的反应产物; （III）使步骤（II）的氧化产物与有机磺酰卤或有机磺酰酐反应; 和（IV）使步骤（III）的反应产物与N-甲基-N-甲磺酰胺反应。

4. 发明申请

US20110160455A1 Preparation of Aminopyrimidine Compounds 有权
标题翻译：氨基嘧啶化合物的制备
公开(公告)号：US20110160455A1
公开(公告)日：2011-06-30
申请号：US12889186
申请日：2010-09-23
申请人： Akio Matsushita , Mizuho Oda , Yasuhiro Kawachi , Jun-ichi Chika
发明人： Akio Matsushita , Mizuho Oda , Yasuhiro Kawachi , Jun-ichi Chika
IPC分类号： C07D239/22 , C07D239/42 , C07D239/30
CPC分类号： C07D239/22 , C07D239/30 , C07D239/34 , C07D239/36 , C07D239/42
摘要： A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.
摘要翻译：通过以下步骤制备式（3）的2-（N-甲基-N-甲磺酰基氨基）嘧啶化合物：[R是烃基]：（I）使异丁酰乙酸酯与4-氟苯甲醛和尿素反应质子化合物和金属盐的存在; （II）氧化步骤（I）的反应产物; （III）使步骤（II）的氧化产物与有机磺酰卤或有机磺酰酐反应; 和（IV）使步骤（III）的反应产物与N-甲基-N-甲磺酰胺反应。

5. 发明申请

US20080058520A1 Preparation of Aminopyrimidine Compounds 有权
标题翻译：氨基嘧啶化合物的制备
公开(公告)号：US20080058520A1
公开(公告)日：2008-03-06
申请号：US11933626
申请日：2007-11-01
申请人： Akio Matsushita , Mizuho ODA , Yasuhiro KAWACHI , Jun-ichi CHIKA
发明人： Akio Matsushita , Mizuho ODA , Yasuhiro KAWACHI , Jun-ichi CHIKA
IPC分类号： C07D239/36
CPC分类号： C07D239/22 , C07D239/30 , C07D239/34 , C07D239/36 , C07D239/42
摘要： A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.
摘要翻译：通过以下步骤制备式（3）的2-（N-甲基-N-甲磺酰基氨基）嘧啶化合物：[R是烃基]：（I）使异丁酰乙酸酯与4-氟苯甲醛和尿素反应质子化合物和金属盐的存在; （II）氧化步骤（I）的反应产物; （III）使步骤（II）的氧化产物与有机磺酰卤或有机磺酰酐反应; 和（IV）使步骤（III）的反应产物与N-甲基-N-甲磺酰胺反应。

6. 发明授权

US07304156B2 Preparation of aminopyrimidine compounds 有权
标题翻译：氨基嘧啶化合物的制备
公开(公告)号：US07304156B2
公开(公告)日：2007-12-04
申请号：US10483430
申请日：2002-07-12
申请人： Akio Matsushita , Mizuho Oda , Yasuhiro Kawachi , Jun-ichi Chika
发明人： Akio Matsushita , Mizuho Oda , Yasuhiro Kawachi , Jun-ichi Chika
IPC分类号： C07D239/42 , C07D239/34 , C07D239/22 , A61K31/505 , A61P3/06
CPC分类号： C07D239/22 , C07D239/30 , C07D239/34 , C07D239/36 , C07D239/42
摘要： A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.
摘要翻译：通过以下步骤制备式（3）的2-（N-甲基-N-甲磺酰基氨基）嘧啶化合物：[R是烃基]：（I）使异丁酰乙酸酯与4-氟苯甲醛和尿素反应质子化合物和金属盐的存在; （II）氧化步骤（I）的反应产物; （III）使步骤（II）的氧化产物与有机磺酰卤或有机磺酰酐反应; 和（IV）使步骤（III）的反应产物与N-甲基-N-甲磺酰胺反应。

7. 发明申请

US20120277432A1 Preparation of Aminopyrimidine Compounds 有权
标题翻译：氨基嘧啶化合物的制备
公开(公告)号：US20120277432A1
公开(公告)日：2012-11-01
申请号：US13523534
申请日：2012-06-14
申请人： Akio Matsushita , Mizuho Oda , Yasuhiro Kawachi , Jun-ichi Chika
发明人： Akio Matsushita , Mizuho Oda , Yasuhiro Kawachi , Jun-ichi Chika
IPC分类号： C07D239/42 , C07D239/34 , C07D239/30
CPC分类号： C07D239/22 , C07D239/30 , C07D239/34 , C07D239/36 , C07D239/42
摘要： A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.
摘要翻译：通过以下步骤制备式（3）的2-（N-甲基-N-甲磺酰基氨基）嘧啶化合物：[R是烃基]：（I）使异丁酰乙酸酯与4-氟苯甲醛和尿素反应质子化合物和金属盐的存在; （II）氧化步骤（I）的反应产物; （III）使步骤（II）的氧化产物与有机磺酰卤或有机磺酰酐反应; 和（IV）使步骤（III）的反应产物与N-甲基-N-甲磺酰胺反应。

8. 发明申请

US20090137822A1 Process for preparing 3-substituted thiophene 审中-公开
标题翻译：制备3-取代噻吩的方法
公开(公告)号：US20090137822A1
公开(公告)日：2009-05-28
申请号：US11920568
申请日：2006-05-16
申请人： Akio Matsushita , Kiyotaka Yoshii , Mizuho Oda , Masayoshi Oue , Shuji Yamada
发明人： Akio Matsushita , Kiyotaka Yoshii , Mizuho Oda , Masayoshi Oue , Shuji Yamada
IPC分类号： C07D333/38 , C07D333/22 , C07D333/16
CPC分类号： C07D333/38 , C07D333/22
摘要： The present invention relates to a process for preparing a 3-substituted thiophene represented by the formula (2): wherein R represents a cyano group, a formyl group, a carboxyl group, a hydrocarbyloxycarbonyl group which may have a substituent(s) or an acyl group which may have a substituent(s), which comprises reacting a vinyl compound represented by the formula (1): RCH═CHY (1) wherein R has the same meaning as defined above, and Y represents a leaving group, and an α-mercaptoacetaldehyde or a multimer thereof.
摘要翻译：本发明涉及一种由式（2）表示的3-取代噻吩的制备方法：其中R表示氰基，甲酰基，羧基，可具有取代基的烃氧基羰基或可以具有取代基的酰基，其包括使由式（1）表示的乙烯基化合物：<？in-line-formula description =“In-line formula”end =“lead”→RCH-CHY （1）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中R具有与上述相同的含义，Y表示离去基团，而α-巯基乙醛或多聚体其中。

9. 发明授权

US5677455A Preparation of 3-oxy-5-oxo-6-heptenoic acid derivatives 失效
标题翻译： 3-氧基-5-氧代-6-庚烯酸衍生物的制备
公开(公告)号：US5677455A
公开(公告)日：1997-10-14
申请号：US524045
申请日：1995-09-06
申请人： Katsumasa Harada , Akio Matsushita , Yasuhiro Kawachi , Hiroshi Sasaki
发明人： Katsumasa Harada , Akio Matsushita , Yasuhiro Kawachi , Hiroshi Sasaki
IPC分类号： C07F7/18 , C07F7/02 , C07D213/30
CPC分类号： C07F7/1852 , C07F7/1856 , C07F7/1892
摘要： Methyl (3R,6E)-3-�(tert-butyldimethylsilyl)oxy!-7-�2',6'-diisopropyl-4'-(4"-fluorophenyl)-5'-(methoxymethyl)pyridin-3'-yl!-5-oxy-6-heptenoate or other 3-oxy-5-oxo-6-heptenoic acid derivative is prepared by the reaction of an aromatic aldehyde and an oxyglutaric acid derivative in an aliphatic alcohol containing a small amount of water in the presence of an alkali metal carbonate or hydrogen carbonate.
摘要翻译：将（3R，6E）-3 - [（叔丁基二甲基甲硅烷基）氧基] -7- [2'，6'-二异丙基-4' - （4“ - 氟苯基）-5' - （甲氧基甲基） - 基] -5-氧基-6-庚烯酸乙酯或其它3-氧基-5-氧代-6-庚烯酸衍生物通过芳族醛和羟基戊二酸衍生物在含少量水的脂族醇中的反应来制备在碱金属碳酸盐或碳酸氢盐存在下进行。

10. 发明授权

US5892126A Process for preparing 4-fluoro-3-trifluoromethylphenol 失效
标题翻译：制备4-氟-3-三氟甲基苯酚的方法
公开(公告)号：US5892126A
公开(公告)日：1999-04-06
申请号：US969692
申请日：1997-11-13
申请人： Katsumasa Harada , Akio Matsushita , Yasuhiro Kawachi
发明人： Katsumasa Harada , Akio Matsushita , Yasuhiro Kawachi
IPC分类号： C07C39/26 , C07C39/24
CPC分类号： C07C39/26
摘要： Disclosed is a process for preparing 4-fluoro-3-trifluoromethylphenol from 4-fluoro-3-trifluoromethylaniline, which comprises the steps of (1) using about 1 to 20 parts by weight of water based on 1 part by weight of 4-fluoro-3-trifluoromethylaniline in the presence of sulfuric acid to obtain 4-fluoro-3-trifluoromethylaniline sulfate; (2) subjecting the obtained 4-fluoro-3-trifluoromethylaniline sulfate to a diazotization reaction by using a diazotizing agent to obtain an aqueous solution containing about 8 to 25% by weight of a 4-fluoro-3-trifluoromethylbenzene-diazonium salt where a sulfuric acid concentration after diazotization is about 30 to 70% by weight in terms of the amount of sulfuric acid added, and the amount of water used is about 1 to 20 parts by weight based on 1 part by weight of 4-fluoro-3-trifluoromethylaniline; and (3) hydrolyzing the obtained 4-fluoro-3-trifluoromethylbenzenediazonium salt where a sulfuric acid concentration is about 30 to 70% by weight in terms of the amount of sulfuric acid added in a copper sulfate aqueous solution.
摘要翻译：公开了从4-氟-3-三氟甲基苯胺制备4-氟-3-三氟甲基苯酚的方法，其包括以下步骤：（1）使用约1至20重量份的水，基于1重量份的4-氟 -3-三氟甲基苯胺在硫酸存在下反应，得到4-氟-3-三氟甲基苯胺硫酸盐; （2）通过使用重氮化试剂使得到的4-氟-3-三氟甲基苯胺硫酸盐进行重氮化反应，得到含有约8-25重量％的4-氟-3-三氟甲基苯 - 重氮盐的水溶液，其中重氮化后的硫酸浓度以加入的硫酸的量计为约30〜70重量％，相对于1重量份的4-氟-3-甲基丙烯酸，使用的水的量为约1〜20重量份，三氟甲基苯胺; 和（3）水解所得到的硫酸浓度为硫酸铜水溶液中加入的硫酸的量的约30〜70重量％的4-氟-3-三氟甲基苯二氮鎓盐。

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