公开(公告)号：US5538995A

公开(公告)日：1996-07-23

申请号：US390316

申请日：1995-02-17

申请人： Yasushi Matsumura ,  Takashi Nakano ,  Mayumi Makino ,  Yoshitomi Morizawa

发明人： Yasushi Matsumura ,  Takashi Nakano ,  Mayumi Makino ,  Yoshitomi Morizawa

IPC分类号： C07D307/93 ,  C07D307/935 ,  C07D307/937 ,  C07D407/12 ,  C07D493/08 ,  C07F7/18 ,  A61K31/34

CPC分类号： C07D307/935 ,  C07D307/937 ,  C07D493/08 ,  C07F7/1856 ,  C07F7/1892 ,  Y02P20/55

摘要： A difluoroprostacyclin of the following formula (V), its lower alkanol ester or its pharmaceutically acceptable salt: ##STR1## wherein A is an ethylene group, a vinylene group or an ethynylene group, R is a substituted or unsubstituted C.sub.1-10 alkyl group, a substituted or unsubstituted C.sub.1-10 alkenyl group, a substituted or unsubstituted C.sub.1-10 alkynyl group, a substituted or unsubstituted C.sub.3-8 cycloalkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryloxy group, Q is a substituted or unsubstituted C.sub.1-10 alkyl group, a substituted or unsubstituted C.sub.1-10 alkenyl group, a substituted or unsubstituted C.sub.1-10 alkynyl group, a substituted or unsubstituted C.sub.3-8 cycloalkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group.

摘要翻译： （V）的二氟前列环素，其低级烷醇酯或其药学上可接受的盐：其中A是亚乙基，亚乙烯基或亚乙炔基，R是取代或未取代的C1-10 取代或未取代的C1-10链烯基，取代或未取代的C1-10炔基，取代或未取代的C3-8环烷基，取代或未取代的芳烷基或取代或未取代的芳氧基，Q是 取代或未取代的C1-10烷基，取代或未取代的C1-10烯基，取代或未取代的C1-10炔基，取代或未取代的C3-8环烷基，取代或未取代的芳烷基或取代 或未取代的芳基。

公开(公告)号：US20080255385A1

公开(公告)日：2008-10-16

申请号：US12139553

申请日：2008-06-16

申请人： Mayumi Makino ,  Kazuhisa Sakata ,  Yasushi Matsumura

发明人： Mayumi Makino ,  Kazuhisa Sakata ,  Yasushi Matsumura

IPC分类号： C07C69/65 ,  C07C209/68 ,  C07C57/03

CPC分类号： C07C229/26 ,  C07B57/00 ,  C07B2200/07 ,  C07C51/487 ,  C07C57/52

摘要： To provide a method for producing an optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid, a basic amino acid salt thereof or an optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid ester with high yield and high optical purity by simple operation.An optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid is obtained by precipitating a basic amino acid salt of optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid from a solvent solution containing an optical isomer mixture of (4E)-5-chloro-2-isopropyl-4-pentenoic acid and an optically active basic amino acid or a salt thereof, and then the basic amino acid salt of optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid is subjected to a desalting reaction. Further, an esterification reaction is carried out to obtain an optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid ester.

摘要翻译： 为了提供一种制备光学活性（4E）-5-氯-2-异丙基-4-戊烯酸，其碱性氨基酸盐或光学活性（4E）-5-氯-2-异丙基-4-戊烯酸的方法， 戊烯酸酯，产率高，光学纯度高。 通过从溶剂中沉淀光学活性（4E）-5-氯-2-异丙基-4-戊烯酸的碱性氨基酸盐获得光学活性（4E）-5-氯-2-异丙基-4-戊烯酸 （4E）-5-氯-2-异丙基-4-戊烯酸和光学活性碱性氨基酸或其盐的光学异构体混合物，然后将光学活性（4E）-5的碱性氨基酸盐 - 氯-2-异丙基-4-戊烯酸进行脱盐反应。 此外，进行酯化反应以获得光学活性（4E）-5-氯-2-异丙基-4-戊烯酸酯。

公开(公告)号：US5747531A

公开(公告)日：1998-05-05

申请号：US741905

申请日：1996-10-31

申请人： Yasushi Matsumura ,  Takashi Nakano ,  Mayumi Makino ,  Yoshitomi Morizawa

发明人： Yasushi Matsumura ,  Takashi Nakano ,  Mayumi Makino ,  Yoshitomi Morizawa

IPC分类号： C07D307/93 ,  C07D307/935 ,  C07D307/937 ,  C07D407/12 ,  C07D493/08 ,  C07F7/18 ,  A01N43/08

CPC分类号： C07D307/935 ,  C07D307/937 ,  C07D493/08 ,  C07F7/1856 ,  C07F7/1892 ,  Y02P20/55

摘要： A difluoroprostacyclin of the following formula (V), its lower alkanol ester or its pharmaceutically acceptable salt: ##STR1## wherein A is an ethylene group, a vinylene group or an ethynylene group, R is a substituted or unsubstituted C.sub.1-10 alkyl group, a substituted or unsubstituted C.sub.1-10 alkenyl group, a substituted or unsubstituted C.sub.1-10 alkynyl group, a substituted or unsubstituted C.sub.3-8 cycloalkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryloxy group, Q is a substituted or unsubstituted C.sub.1-10 alkyl group, a substituted or unsubstituted C.sub.1-10 alkenyl group, a substituted or unsubstituted C.sub.1-10 alkynyl group, a substituted or unsubstituted C.sub.3-8 cycloalkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group.

公开(公告)号：US5616732A

公开(公告)日：1997-04-01

申请号：US600824

申请日：1996-02-13

申请人： Yasushi Matsumura ,  Takashi Nakano ,  Mayumi Makino ,  Yoshitomi Morizawa

发明人： Yasushi Matsumura ,  Takashi Nakano ,  Mayumi Makino ,  Yoshitomi Morizawa

IPC分类号： C07D307/93 ,  C07D307/935 ,  C07D307/937 ,  C07D407/12 ,  C07D493/08 ,  C07F7/18

CPC分类号： C07D307/935 ,  C07D307/937 ,  C07D493/08 ,  C07F7/1856 ,  C07F7/1892 ,  Y02P20/55

摘要： A difluoroprostacyclin of the following formula (V), its lower alkanol ester or its pharmaceutically acceptable salt: ##STR1## wherein A is an ethylene group, a vinylene group or an ethynylene group, R is a substituted or unsubstituted C.sub.1-10 alkyl group, a substituted or unsubstituted C.sub.1-10 alkenyl group, a substituted or unsubstituted C.sub.1-10 alkynyl group, a substituted or unsubstituted C.sub.3-8 cycloalkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryloxy group, Q is a substituted or unsubstituted C.sub.1-10 alkyl group, a substituted or unsubstituted C.sub.1-10 alkenyl group, a substituted or unsubstituted C.sub.1-10 alkynyl group, a substituted or unsubstituted C.sub.3-8 cycloalkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group.

摘要翻译： （V）的二氟前列环素，其低级烷醇酯或其药学上可接受的盐：其中A是亚乙基，亚乙烯基或亚乙炔基，R是取代或未取代的C1-10 取代或未取代的C1-10链烯基，取代或未取代的C1-10炔基，取代或未取代的C3-8环烷基，取代或未取代的芳烷基或取代或未取代的芳氧基，Q是 取代或未取代的C1-10烷基，取代或未取代的C1-10烯基，取代或未取代的C1-10炔基，取代或未取代的C3-8环烷基，取代或未取代的芳烷基或取代 或未取代的芳基。