公开(公告)号：US09278938B2

公开(公告)日：2016-03-08

申请号：US14123381

申请日：2012-06-14

申请人： Yoichi Kawabata ,  Yasuhiro Sawai ,  Kazuaki Kanno ,  Naotaka Sawada

发明人： Yoichi Kawabata ,  Yasuhiro Sawai ,  Kazuaki Kanno ,  Naotaka Sawada

IPC分类号： C07D233/64 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07D233/64

摘要： The present invention provides an advantageous production method of an imidazole derivative, which is suitable for industrial production.Compound (VI) is produced by reacting compound (I) with a Grignard reagent or a magnesium reagent, and a lithium reagent, and then reacting the resulting compound with compound (V).

摘要翻译： 本发明提供了适用于工业生产的咪唑衍生物的有利制备方法。 化合物（VI）通过使化合物（I）与格氏试剂或镁试剂和锂试剂反应，然后使所得化合物与化合物（V）反应来制备。

公开(公告)号：US20140100373A1

公开(公告)日：2014-04-10

申请号：US14123381

申请日：2012-06-14

申请人： Yoichi Kawabata ,  Yasuhiro Sawai ,  Kazuaki Kanno ,  Naotaka Sawada

发明人： Yoichi Kawabata ,  Yasuhiro Sawai ,  Kazuaki Kanno ,  Naotaka Sawada

IPC分类号： C07D233/64 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07D233/64

摘要： The present invention provides an advantageous production method of an imidazole derivative, which is suitable for industrial production.Compound (VI) is produced by reacting compound (I) with a Grignard reagent or a magnesium reagent, and a lithium reagent, and then reacting the resulting compound with compound (V).

摘要翻译： 本发明提供了适用于工业生产的咪唑衍生物的有利制备方法。 化合物（VI）通过使化合物（I）与格氏试剂或镁试剂和锂试剂反应，然后使所得化合物与化合物（V）反应来制备。

公开(公告)号：US06531594B2

公开(公告)日：2003-03-11

申请号：US09933007

申请日：2001-08-21

申请人： Michi Watanabe ,  Takeshi Nakato ,  Jun Takehara ,  Kazuaki Kanno ,  Shuji Ichikawa

发明人： Michi Watanabe ,  Takeshi Nakato ,  Jun Takehara ,  Kazuaki Kanno ,  Shuji Ichikawa

IPC分类号： C07D47720

CPC分类号： C07D207/416 ,  C07D207/14 ,  C07D471/04 ,  C07D477/02 ,  C07D477/20 ,  Y02P20/55

摘要： A process for producing 1H-3-aminopyrrolidine and derivatives thereof is disclosed. The process is especially useful for producing optically active 1H-3-aminopyrrolidine and derivatives thereof and in this case comprises reacting an optically active amino-protected aspartic anhydride represented by the formula (1) with a primary amine represented by the formula R′NH2, subjecting the reaction product to cyclodehydration to obtain an optically active 1-aralkyl-3-(protected amino)pyrrolidine-2,5-dione compound represented by the formula (2), subsequently eliminating the protective group from the 3-position amino group of the compound represented by the formula (2) to obtain an optically active 1-aralkyl-3-aminopyrrolidine-2,5-dione compound represented by the formula (3), reducing the carbonyl groups of the compound represented by the formula (3) to obtain either an optically active 1-aralkyl-3-aminopyrrolidine compound represented by the formula (4) or a salt thereof with a protonic acid, and then subjecting the compound represented by the formula (4) or the salt thereof to hydrogenolysis to obtain an optically active 1H-3-aminopyrrolidine or a protonic acid salt thereof.

摘要翻译： 公开了一种制备1H-3-氨基吡咯烷及其衍生物的方法。 该方法对于制备光学活性的1H-3-氨基吡咯烷及其衍生物特别有用，在这种情况下，包括将由式（1）表示的光学活性的氨基保护的天冬氨酸酐与由式R'NH 2表示的伯胺反应， 使反应产物进行环化脱水，得到由式（2）表示的光学活性1-芳烷基-3-（保护氨基）吡咯烷-2,5-二酮化合物，随后从3-位氨基 由式（2）表示的化合物，得到由式（3）表示的光学活性1-芳烷基-3-氨基吡咯烷-2,5-二酮化合物，还原由式（3）表示的化合物的羰基， 得到由式（4）表示的光学活性1-芳烷基-3-氨基吡咯烷化合物或其盐与质子酸反应，然后使由式（4）表示的化合物或其盐 f进行氢解以获得光学活性的1H-3-氨基吡咯烷或其质子酸盐。

公开(公告)号：US07659409B2

公开(公告)日：2010-02-09

申请号：US10944055

申请日：2004-09-20

申请人： Jun Takehara ,  Jingping Qu ,  Kazuaki Kanno ,  Hiroshi Kawabata ,  Yasumasa Dekishima ,  Makoto Ueda ,  Kyoko Endo ,  Takeshi Murakami ,  Tomoko Sasaki ,  Hisatoshi Uehara ,  Youichi Matsumoto ,  Shihomi Suzuki

发明人： Jun Takehara ,  Jingping Qu ,  Kazuaki Kanno ,  Hiroshi Kawabata ,  Yasumasa Dekishima ,  Makoto Ueda ,  Kyoko Endo ,  Takeshi Murakami ,  Tomoko Sasaki ,  Hisatoshi Uehara ,  Youichi Matsumoto ,  Shihomi Suzuki

IPC分类号： C07D333/22

CPC分类号： C07D333/16 ,  B01J31/1805 ,  B01J31/2295 ,  B01J2231/643 ,  B01J2531/80 ,  B01J2531/821

摘要： The object of the present invention is to provide 3-hydroxy-3-(2-thienyl)propionamides useful as synthesis intermediates of pharmaceutical preparations and the like and a method for obtaining optically active 3-amino-1-(2-thienyl)-1-propanols using the same with high reaction yield, high optical yield and industrially low cost.According to the present invention, 3-amino-1-(2-thienyl)-1-propanols are obtained by carrying out asymmetric reduction of a β-ketocarbonyl compound having thiophene ring in the presence of a catalyst constituted from a compound of a group VIII or IX metal in the periodic table (e.g., a ruthenium compound) and an asymmetric ligand represented by a specified optically active diamine derivative (e.g., a diphenylethylenediamine derivative), or using a cell, a treated product of said cell or the like of a microorganism, and as occasion demands, carrying out amidation of the ester group and then carrying out reduction of the amido group. (each of the substituents is as described in claim 1).

摘要翻译： 本发明的目的是提供可用作药物制剂等的合成中间体的3-羟基-3-（2-噻吩基）丙酰胺和获得光学活性3-氨基-1-（2-噻吩基） 使用相同的1-丙醇，反应产率高，光学收率高，工业成本低。 根据本发明，3-氨基-1-（2-噻吩基）-1-丙醇通过在由组合的化合物构成的催化剂存在下进行具有噻吩环的β-酮羰基化合物的不对称还原而得到 VIII或IX族金属（例如钌化合物）和由特定光学活性二胺衍生物（例如二苯基乙二胺衍生物）表示的不对称配体，或使用电池，所述电池等的处理产物 微生物，根据需要，进行酯基的酰胺化，然后进行酰胺基的还原。 （每个取代基如权利要求1所述）。

公开(公告)号：US08445731B2

公开(公告)日：2013-05-21

申请号：US13187066

申请日：2011-07-20

申请人： Susumu Tsutsuminai ,  Kazuaki Kanno ,  Makiko Tachikura

发明人： Susumu Tsutsuminai ,  Kazuaki Kanno ,  Makiko Tachikura

IPC分类号： C07C39/12

CPC分类号： C07C37/20 ,  B01J31/10 ,  B01J2231/347 ,  C07D213/32 ,  C07C39/16

摘要： Provided is a process for producing a bisphenol compound stably at a high conversion and with high selectivity over a long period. A process for producing a bisphenol compound by feeding a phenol compound and a carbonyl compound continuously to a reactor packed with an acid catalyst, characterized in that the acid catalyst is a sulfonic-acid-form cation-exchange resin in which part of the sulfo groups have been modified with at least any one of 2-pyridylalkanethiol compounds and 3-pyridylalkanethiol compounds.

摘要翻译： 提供了以高转化率和高选择性长时间稳定生产双酚化合物的方法。 一种通过将酚化合物和羰基化合物连续地加入到装有酸催化剂的反应器中生产双酚化合物的方法，其特征在于酸催化剂是磺酸型阳离子交换树脂，其中部分磺基 已经用2-吡啶基烷硫醇化合物和3-吡啶基烷硫醇化合物中的至少一种进行了改性。

公开(公告)号：US20120010434A1

公开(公告)日：2012-01-12

申请号：US13187066

申请日：2011-07-20

申请人： Susumu Tsutsuminai ,  Kazuaki Kanno ,  Makiko Tachikura

发明人： Susumu Tsutsuminai ,  Kazuaki Kanno ,  Makiko Tachikura

IPC分类号： C07C37/20

CPC分类号： C07C37/20 ,  B01J31/10 ,  B01J2231/347 ,  C07D213/32 ,  C07C39/16

摘要： Provided is a process for producing a bisphenol compound stably at a high conversion and with high selectivity over a long period. A process for producing a bisphenol compound by feeding a phenol compound and a carbonyl compound continuously to a reactor packed with an acid catalyst, characterized in that the acid catalyst is a sulfonic-acid-form cation-exchange resin in which part of the sulfo groups have been modified with at least any one of 2-pyridylalkanethiol compounds and 3-pyridylalkanethiol compounds.

摘要翻译： 提供了以高转化率和高选择性长时间稳定生产双酚化合物的方法。 一种通过将酚化合物和羰基化合物连续地加入到装有酸催化剂的反应器中生产双酚化合物的方法，其特征在于酸催化剂是磺酸型阳离子交换树脂，其中部分磺基 已经用2-吡啶基烷硫醇化合物和3-吡啶基烷硫醇化合物中的至少一种进行了改性。

公开(公告)号：US20050107621A1

公开(公告)日：2005-05-19

申请号：US10944055

申请日：2004-09-20

申请人： Jun Takehara ,  Jingping Qu ,  Kazuaki Kanno ,  Hiroshi Kawabata ,  Yasumasa Dekishima ,  Makoto Ueda ,  Kyoko Endo ,  Takeshi Murakami ,  Tomoko Sasaki ,  Hisatoshi Uehara ,  Youichi Matsumoto ,  Shihomi Suzuki

发明人： Jun Takehara ,  Jingping Qu ,  Kazuaki Kanno ,  Hiroshi Kawabata ,  Yasumasa Dekishima ,  Makoto Ueda ,  Kyoko Endo ,  Takeshi Murakami ,  Tomoko Sasaki ,  Hisatoshi Uehara ,  Youichi Matsumoto ,  Shihomi Suzuki

IPC分类号： A61K31/381 ,  C07D333/16 ,  C07D333/22

CPC分类号： C07D333/16 ,  B01J31/1805 ,  B01J31/2295 ,  B01J2231/643 ,  B01J2531/80 ,  B01J2531/821

摘要： The object of the present invention is to provide 3-hydroxy-3-(2-thienyl)propionamides useful as synthesis intermediates of pharmaceutical preparations and the like and a method for obtaining optically active 3-amino-1-(2-thienyl)-1-propanols using the same with high reaction yield, high optical yield and industrially low cost. According to the present invention, 3-amino-1-(2-thienyl)-1-propanols are obtained by carrying out asymmetric reduction of a β-ketocarbonyl compound having thiophene ring in the presence of a catalyst constituted from a compound of a group VIII or IX metal in the periodic table (e.g., a ruthenium compound) and an asymmetric ligand represented by a specified optically active diamine derivative (e.g., a diphenylethylenediamine derivative), or using a cell, a treated product of said cell or the like of a microorganism, and as occasion demands, carrying out amidation of the ester group and then carrying out reduction of the amido group. (each of the substituents is as described in claim 1).

摘要翻译： 本发明的目的是提供可用作药物制剂等的合成中间体的3-羟基-3-（2-噻吩基）丙酰胺和获得光学活性3-氨基-1-（2-噻吩基） 使用相同的1-丙醇，反应产率高，光学收率高，工业成本低。 根据本发明，3-氨基-1-（2-噻吩基）-1-丙醇通过在由组合的化合物构成的催化剂存在下进行具有噻吩环的β-酮羰基化合物的不对称还原而得到 VIII或IX族金属（例如钌化合物）和由特定光学活性二胺衍生物（例如二苯基乙二胺衍生物）表示的不对称配体，或使用电池，所述电池等的处理产物 微生物，根据需要，进行酯基的酰胺化，然后进行酰胺基的还原。 （每个取代基如权利要求1所述）。