公开(公告)号：US07414136B2

公开(公告)日：2008-08-19

申请号：US11265179

申请日：2005-11-03

申请人： Yasushi Matsumura ,  Nobuaki Mori ,  Yasuhiro Yamada

发明人： Yasushi Matsumura ,  Nobuaki Mori ,  Yasuhiro Yamada

IPC分类号： C07D213/85 ,  C07D213/80

CPC分类号： C07D213/80

摘要： To provide a method for producing a 3-substituted 2-chloro-5-fluoro-pyridine or its salt in high yield from a readily available material through a short process under mild reaction conditions using a reagent which is easy for handling and simple in the reaction operation. Namely, a method for producing the following compound (2) or its salt which comprises selectively reducing a chlorine atom at the 6-position of the following compound (1) or its salt, is provided. Further, a method for producing the following compound (4) or its salt which comprises substituting a Z1 group of the following compound (2) or its salt obtained by the reduction reaction, by a Z2 group, is provided. Here, Z1 is —CO2R1, etc., and R1 is a hydrogen atom, an alkyl group, an alkenyl group, an aryl group, an aralkyl group or a cycloalkyl group. Z2 is a group different from Z1 and is —CO2R5, etc., and R5 is an alkyl group, an alkenyl group, an aryl group, an aralkyl group or a cycloalkyl group.

摘要翻译： 提供一种通过使用容易处理的试剂在温和的反应条件下通过短时间过程从容易获得的材料以高产率制备3-取代的2-氯-5-氟 - 吡啶或其盐的方法， 反应操作。 即，提供了下述化合物（1）或其盐选择性还原6-位的氯原子的下述化合物（2）或其盐的制造方法。 此外，制备下列化合物（4）或其盐的方法，该方法包括用下列化合物（2）或其还原反应得到的盐代替Z ^{2 组。 这里，Z 1是-CO 2 R 1等，R 1是氢原子， 烷基，烯基，芳基，芳烷基或环烷基。 Z 2是与Z 1不同的基团，并且是-CO 2 R 5等，R 2 烷基，烯基，芳基，芳烷基或环烷基。}

公开(公告)号：US20060058529A1

公开(公告)日：2006-03-16

申请号：US11265179

申请日：2005-11-03

申请人： Yasushi Matsumura ,  Nobuaki Mori ,  Yasuhiro Yamada

发明人： Yasushi Matsumura ,  Nobuaki Mori ,  Yasuhiro Yamada

IPC分类号： C07D213/84 ,  C07D213/46

CPC分类号： C07D213/80

摘要： To provide a method for producing a 3-substituted 2-chloro-5-fluoro-pyridine or its salt in high yield from a readily available material through a short process under mild reaction conditions using a reagent which is easy for handling and simple in the reaction operation. Namely, a method for producing the following compound (2) or its salt which comprises selectively reducing a chlorine atom at the 6-position of the following compound (1) or its salt, is provided. Further, a method for producing the following compound (4) or its salt which comprises substituting a Z1 group of the following compound (2) or its salt obtained by the reduction reaction, by a Z2 group, is provided. Here, Z1 is —CO2R1, etc., and R1 is a hydrogen atom, an alkyl group, an alkenyl group, an aryl group, an aralkyl group or a cycloalkyl group. Z2 is a group different from Z1 and is —CO2R5, etc., and R5 is an alkyl group, an alkenyl group, an aryl group, an aralkyl group or a cycloalkyl group.

摘要翻译： 提供一种通过使用容易处理的试剂在温和的反应条件下通过短时间过程从容易获得的材料以高产率制备3-取代的2-氯-5-氟 - 吡啶或其盐的方法， 反应操作。 即，提供了下述化合物（1）或其盐选择性还原6-位的氯原子的下述化合物（2）或其盐的制造方法。 此外，制备下列化合物（4）或其盐的方法，该方法包括用下列化合物（2）或其还原反应得到的盐代替Z ^{2 组。 这里，Z 1是-CO 2 R 1等，R 1是氢原子， 烷基，烯基，芳基，芳烷基或环烷基。 Z 2是与Z 1不同的基团，并且是-CO 2 R 5等，R 2 5是烷基，烯基，芳基，芳烷基或环烷基环}

公开(公告)号：US07232925B2

公开(公告)日：2007-06-19

申请号：US11147255

申请日：2005-06-08

申请人： Nobuaki Mori ,  Yasushi Matsumura ,  Yoshitomi Morizawa ,  Toshihiko Kaminuma ,  Yuuichi Aoki

发明人： Nobuaki Mori ,  Yasushi Matsumura ,  Yoshitomi Morizawa ,  Toshihiko Kaminuma ,  Yuuichi Aoki

IPC分类号： C07C69/62

CPC分类号： C07C67/343 ,  C07B2200/07 ,  C07B2200/09 ,  C07C67/32 ,  C07C67/48 ,  C07C69/65

摘要： The present invention provides processes for producing a (4E)-5-chloro-2-isopropyl-4-pentenoate and an optical isomer of the (4E)-5-chloro-2-isopropyl-4-pentenoate, namely a process for producing a (4E)-5-chloro-2-isopropyl-4-pentenoate represented by the following formula (4), which comprises reacting a compound represented by the following formula (2) in the presence of an aprotic solvent (II) with a base (II) and then with (1E)-1,3-dichloro-1-propene to give a compound represented by the following formula (3), and dealkoxycarbonylating either ester in the compound represented by the following formula (3), and a process for producing a (S)-(4E)-5-chloro-2-isopropyl-4-pentenoate represented by the following formula (5), which comprises optically resolving a (4E)-5-chloro-2-isopropyl-4-pentenoate represented by the formula (4) obtained by the above-mentioned process (wherein R is a lower alkyl group or an aralkyl group).

摘要翻译： 本发明提供了（4E）-5-氯-2-异丙基-4-戊烯酸酯和（4E）-5-氯-2-异丙基-4-戊烯酸酯的旋光异构体的制备方法，即制备 由下式（4）表示的（4E）-5-氯-2-异丙基-4-戊烯酸酯，其包括使下式（2）表示的化合物在非质子溶剂（II）的存在下与 碱（II），然后与（1E）-1,3-二氯-1-丙烯反应，得到由下式（3）表示的化合物，和由下式（3）表示的化合物中的任一酯脱甲基羰基化，和 一种制备由下式（5）表示的（S） - （4E）-5-氯-2-异丙基-4-戊烯酸酯的方法，该方法包括光学拆分（4E）-5-氯-2-异丙基-4-戊烯酸 由上述方法（其中R是低级烷基或芳烷基）得到的式（4）表示的4-戊烯酸酯。

公开(公告)号：US06476228B1

公开(公告)日：2002-11-05

申请号：US09666585

申请日：2000-09-20

申请人： Shu-zhong Wang ,  Takashi Okazoe ,  Yasushi Matsumura ,  Nobuaki Mori ,  Jiro Nishino ,  Kazuhiro Ookura

发明人： Shu-zhong Wang ,  Takashi Okazoe ,  Yasushi Matsumura ,  Nobuaki Mori ,  Jiro Nishino ,  Kazuhiro Ookura

IPC分类号： C07D21140

CPC分类号： C07D211/22 ,  C07C255/41 ,  C07D211/78

摘要： A process for producing a piperidinecarbinol represented by the general formula (2), which comprises reducing the trans isomer of a compound represented by the general formula (1): wherein R1 is a hydrogen atom, a lower alkyl group or an aralkyl group, R2 is a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, and X is a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, a dialkylamino group, an alkylthio group, an arylthio group or CmF2m+1— wherein m is an integer of from 1 to 20.

摘要翻译： 一种制备由通式（2）表示的哌啶甲醇的方法，其包括降低由通式（1）表示的化合物的反式异构体：其中R1是氢原子，低级烷基或芳烷基，R2 是氢原子，低级烷基，芳基或芳烷基，X是氢原子，卤素原子，烷基，芳基，芳烷基，烷氧基，二烷基氨基， 烷硫基，芳硫基或CmF2m + 1-，其中m为1〜20的整数。

公开(公告)号：US06197960B1

公开(公告)日：2001-03-06

申请号：US08835646

申请日：1997-04-11

申请人： Shu-zhong Wang ,  Takashi Okazoe ,  Yasushi Matsumura ,  Nobuaki Mori ,  Jiro Nishino ,  Kazuhiro Ookura

发明人： Shu-zhong Wang ,  Takashi Okazoe ,  Yasushi Matsumura ,  Nobuaki Mori ,  Jiro Nishino ,  Kazuhiro Ookura

IPC分类号： C07D21140

CPC分类号： C07D211/22 ,  C07C255/41 ,  C07D211/78

摘要： A process for producing a piperidinecarbinol represented by the general formula (2), which comprises reducing the trans isomer of a compound represented by the general formula (1): wherein R1 is a hydrogen atom, a lower alkyl group or an aralkyl group, R2 is a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, and X is a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, a dialkylamino group, an alkylthio group, an arylthio group or CmF2m+1— wherein m is an integer of from 1 to 20.

摘要翻译： 一种制备由通式（2）表示的哌啶甲醇的方法，其包括降低由通式（1）表示的化合物的反式异构体：其中R1是氢原子，低级烷基或芳烷基，R2 是氢原子，低级烷基，芳基或芳烷基，X是氢原子，卤素原子，烷基，芳基，芳烷基，烷氧基，二烷基氨基， 烷硫基，芳硫基或CmF2m + 1-，其中m为1〜20的整数。

公开(公告)号：US5985920A

公开(公告)日：1999-11-16

申请号：US127804

申请日：1998-08-03

申请人： Eiichi Shirasawa ,  Masaaki Kageyama ,  Tadashi Nakajima ,  Takashi Nakano ,  Nobuaki Mori ,  Hideshi Sasakura ,  Yasushi Matsumura ,  Yoshitomi Morizawa

发明人： Eiichi Shirasawa ,  Masaaki Kageyama ,  Tadashi Nakajima ,  Takashi Nakano ,  Nobuaki Mori ,  Hideshi Sasakura ,  Yasushi Matsumura ,  Yoshitomi Morizawa

IPC分类号： A61K31/5575 ,  A61K31/557 ,  A61P27/02 ,  A61P27/06 ,  C07C405/00

CPC分类号： C07C405/00 ,  C07C405/0016 ,  C07C405/0033

摘要： A fluorine-containing prostaglandin derivative of the formula (1) (or a salt thereof) and a medicine containing it, particularly, a preventive or therapeutic medicine for an eye disease: ##STR1## wherein A is a vinylene group or the like, R.sup.1 is an aryloxyalkyl group or the like, R.sup.2 and R.sup.3 are hydrogen atoms or the like, and Z is OR.sup.4 (wherein OR.sup.4 is a hydrogen atom or an alkyl group) or the like.

摘要翻译： 式（1）的含氟前列腺素衍生物（或其盐）和含有其的药物，特别是眼部疾病的预防或治疗药物：其中A为亚乙烯基等，R 1为芳氧基烷基 基团等，R2和R3是氢原子等，Z是OR4（其中OR4是氢原子或烷基）等。

公开(公告)号：US06590102B1

公开(公告)日：2003-07-08

申请号：US09721762

申请日：2000-11-27

申请人： Shu-zhong Wang ,  Takashi Okazoe ,  Yasushi Matsumura ,  Nobuaki Mori ,  Jiro Nishino ,  Kazuhiro Ookura

发明人： Shu-zhong Wang ,  Takashi Okazoe ,  Yasushi Matsumura ,  Nobuaki Mori ,  Jiro Nishino ,  Kazuhiro Ookura

IPC分类号： C07D21140

CPC分类号： C07D211/22 ,  C07C255/41 ,  C07D211/78

摘要： A process for producing a piperidinecarbinol represented by the general formula (2), which comprises reducing the trans isomer of a compound represented by the general formula (1): wherein R1 is a hydrogen atom, a lower alkyl group or an aralkyl group, R2 is a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, and X is a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, a dialkylamino group, an alkylthio group, an arylthio group or CmF2m+1— wherein m is an integer of from 1 to 20.

公开(公告)号：US5886035A

公开(公告)日：1999-03-23

申请号：US993017

申请日：1997-12-18

申请人： Eiichi Shirasawa ,  Masaaki Kageyama ,  Tadashi Nakajima ,  Takashi Nakano ,  Nobuaki Mori ,  Hideshi Sasakura ,  Yasushi Matsumura ,  Yoshitomi Morizawa

发明人： Eiichi Shirasawa ,  Masaaki Kageyama ,  Tadashi Nakajima ,  Takashi Nakano ,  Nobuaki Mori ,  Hideshi Sasakura ,  Yasushi Matsumura ,  Yoshitomi Morizawa

IPC分类号： A61K31/5575 ,  A61K31/557 ,  A61P27/02 ,  A61P27/06 ,  C07C405/00

CPC分类号： C07C405/00 ,  C07C405/0016 ,  C07C405/0033

摘要： A fluorine-containing prostaglandin derivative of the formula (1) (or a salt thereof) and a medicine containing it, particularly, a preventive or therapeutic medicine for an eye disease: ##STR1## wherein A is a vinylene group or the like, R.sup.1 is an aryloxyalkyl group or the like, R.sup.2 and R.sup.3 are hydrogen atoms or the like, and Z is OR.sup.4 (wherein OR.sup.4 is a hydrogen atom or an alkyl group) or the like.

摘要翻译： 式（1）的含氟前列腺素衍生物（或其盐）和含有它的药物，特别是眼部疾病的预防或治疗药物：（1）其中A是亚乙烯基或 类似地，R 1是芳氧基烷基等，R 2和R 3是氢原子等，Z是OR 4（其中OR 4是氢原子或烷基）等。

公开(公告)号：US20050228193A1

公开(公告)日：2005-10-13

申请号：US11147255

申请日：2005-06-08

申请人： Nobuaki Mori ,  Yasushi Matsumura ,  Yoshitomi Morizawa ,  Toshihiko Kaminuma ,  Yuuichi Aoki

发明人： Nobuaki Mori ,  Yasushi Matsumura ,  Yoshitomi Morizawa ,  Toshihiko Kaminuma ,  Yuuichi Aoki

IPC分类号： C07C67/32 ,  C07C67/343 ,  C07C67/48 ,  C07C69/62

CPC分类号： C07C67/343 ,  C07B2200/07 ,  C07B2200/09 ,  C07C67/32 ,  C07C67/48 ,  C07C69/65

摘要： The present invention provides processes for producing a (4E)-5-chloro-2-isopropyl-4-pentenoate and an optical isomer of the (4E)-5-chloro-2-isopropyl-4-pentenoate, namely a process for producing a (4E)-5-chloro-2-isopropyl-4-pentenoate represented by the following formula (4), which comprises reacting a compound represented by the following formula (2) in the presence of an aprotic solvent (II) with a base (II) and then with (1E)-1,3-dichloro-1-propene to give a compound represented by the following formula (3), and dealkoxycarbonylating either ester in the compound represented by the following formula (3), and a process for producing a (S)-(4E)-5-chloro-2-isopropyl-4-pentenoate represented by the following formula (5), which comprises optically resolving a (4E)-5-chloro-2-isopropyl-4-pentenoate represented by the formula (4) obtained by the above-mentioned process (wherein R is a lower alkyl group or an aralkyl group).

摘要翻译： 本发明提供了（4E）-5-氯-2-异丙基-4-戊烯酸酯和（4E）-5-氯-2-异丙基-4-戊烯酸酯的旋光异构体的制备方法，即制备 由下式（4）表示的（4E）-5-氯-2-异丙基-4-戊烯酸酯，其包括使下式（2）表示的化合物在非质子溶剂（II）的存在下与 碱（II），然后与（1E）-1,3-二氯-1-丙烯反应，得到由下式（3）表示的化合物，和由下式（3）表示的化合物中的任一酯脱甲基羰基化，和 一种制备由下式（5）表示的（S） - （4E）-5-氯-2-异丙基-4-戊烯酸酯的方法，该方法包括光学拆分（4E）-5-氯-2-异丙基-4-戊烯酸 由上述方法（其中R是低级烷基或芳烷基）得到的式（4）表示的4-戊烯酸酯。

公开(公告)号：US20070191630A1

公开(公告)日：2007-08-16

申请号：US11691873

申请日：2007-03-27

申请人： Toshitsugu Sakaeda ,  Nobuaki Mori ,  Hideto Kanoh

发明人： Toshitsugu Sakaeda ,  Nobuaki Mori ,  Hideto Kanoh

IPC分类号： C07C69/62

CPC分类号： C12P41/005 ,  C07C67/32 ,  C07C67/343 ,  C12P7/62 ,  C07C69/65

摘要： To provide a process for producing a (4E)-5-chloro-2-isopropyl-4-pentenoate in high yield and efficiently. A compound (2) is reacted with a base in the presence of an aprotic solvent and then with (1E)-1,3-dichloro-1-propene in the same reaction vessel to obtain a compound (3), and then either of —COOR moieties in the compound (3) is replaced with a hydrogen atom in the same reaction vessel to obtain a compound (4): wherein R is a lower alkyl group or an aralkyl group.

摘要翻译： 提供以高产率和高效率生产（4E）-5-氯-2-异丙基-4-戊烯酸酯的方法。 化合物（2）在非质子溶剂存在下与碱反应，然后与（1E）-1,3-二氯-1-丙烯在同一反应容器中反应，得到化合物（3），然后 化合物（3）中的-COOR部分被同一反应容器中的氢原子代替，得到化合物（4）：其中R是低级烷基或芳烷基。