公开(公告)号：EP1201663A4

公开(公告)日：2005-02-16

申请号：EP99929773

申请日：1999-07-09

申请人： UBE INDUSTRIES ,  ASTRAZENECA UK LTD

发明人： HARADA KATSUMASA ,  NISHINO SHIGEYOSHI ,  YOSHII KIYOTAKA

IPC分类号： C07D281/16 ,  A61K31/55 ,  A61K31/554 ,  A61P25/18 ,  C07C319/14 ,  C07C323/62 ,  C07B61/00

CPC分类号： C07D281/14 ,  C07C319/14 ,  C07C323/62 ,  C07D281/16

摘要： A process for producing dibenzothiazepine derivatives typified by dibenzo[b,f][1,4]thiazepin-11-one which are usable as the starting material for producing 11-[4-(2-(2-hydroxyethoxy)ethyl)]-1-piperazinyldibenzothiazepine derivatives useful as a psychotropic drug, which comprises reacting a nitrobenzene derivative with a thiosalicylic acid derivative, reducing the thus obtained 2-nitro-2'-carboxy-diphenylsulfide derivative, and then further dehydrating and condensing the thus obtained 2-amino-2'-carboxy-diphenylsulfide derivative.

公开(公告)号：EP1323707A4

公开(公告)日：2005-08-17

申请号：EP01963541

申请日：2001-09-10

申请人： UBE INDUSTRIES

发明人： HARADA KATSUMASA ,  FUKUDA YASUHISA ,  YAMANAKA YOSHINORI ,  MURAKAMI TADASHI ,  HIROTSU KENJI

IPC分类号： C07C255/09 ,  C07C253/00

CPC分类号： C07C255/09

摘要： A novel compound of formula (1), i.e., 4,8-dodecadienedinitrile: (1) (wherein the wavy lines are each a cis or trans linkage); and a process for the production of 4,8-dodecadienedinitrile, characterized by reacting a 2-alkoxy-5,9-cyclododecadienone oxime or a 2-halogeno-5,9-cyclododecadienone oxime with formic acid and hydroxylamine.

摘要翻译： 式（1）的新型化合物，即4,8-十二碳二次甲基：（1）（其中波浪线各自是顺式或反式键）; 以及制备4,8-十二碳二烯二腈的方法，其特征在于使2-烷氧基-5,9-环十二碳二烯酮肟或2-卤代-5,9-环十二碳二烯酮肟与甲酸和羟胺反应。

公开(公告)号：EP1310486A4

公开(公告)日：2005-07-27

申请号：EP01951925

申请日：2001-07-19

申请人： UBE INDUSTRIES

发明人： HARADA KATSUMASA ,  NISHINO SHIGEYOSHI ,  HIROTSU KENJI ,  YOKOYAMA SHUJI ,  TAKAHASHI TAKESHI ,  ODA HIROYUKI

IPC分类号： C07C205/56 ,  C07C255/41 ,  C07D209/32 ,  C07D209/34 ,  C07C201/12 ,  C07C205/26 ,  C07C253/30 ,  C07D209/42

CPC分类号： C07D209/34 ,  C07C201/12 ,  C07C205/56 ,  C07C255/41 ,  C07D209/32

摘要： A process for producing 5-fluorooxyindole, represented by the formula (3) characterized by comprising (A) a first step in which a 2-(5-fluoro-2-nitrophenyl)malonic diester represented by the general formula (1) (wherein R?1 and R2¿ may be the same or different and each represents a group not participating in reactions) is cyclized under reduction conditions to generate a 5-fluorooxyindole-3-carboxylic ester represented by the general formula (2) (wherein R1 is the same as defined above) and (B) a second step in which the 5-fluorooxyindole-3-carboxylic ester is decarboxylated.

公开(公告)号：EP1253147A4

公开(公告)日：2003-05-28

申请号：EP01904315

申请日：2001-02-02

申请人： UBE INDUSTRIES

发明人： HARADA KATSUMASA ,  SHIRAI MASASHI ,  SHIBA KOJI ,  FURUYA TOSHIO

IPC分类号： C07D317/54

CPC分类号： C07D317/54

摘要： A process for preparing piperonal, characterized by comprising the three successive steps: (A) the addition step of reacting 1,2-methylenedioxybenzene with glyoxylic acid in the presence of a strong acid to form 3,4-methylenedioxymandelic acid, (B) the extraction step of adding an organic solvent to the reaction fluid and then neutralizing the resulting fluid with a base to thereby extract 3,4-methylenedioxymandelic acid into the organic solvent and separate the fluid into an organic solvent layer and an aqueous layer, and (C) the oxidation step of removing the aqueous layer, concentrating the organic solvent layer, adding nitric acid to the concentrate, and then making the 3,4-methylenedioxymandelic acid react with the nitric acid to form piperonal.

公开(公告)号：EP1229031A4

公开(公告)日：2003-04-16

申请号：EP00966457

申请日：2000-10-13

申请人： UBE INDUSTRIES

发明人： HARADA KATSUMASA ,  SHIRAI MASASHI ,  SHIBA KOJI

IPC分类号： C07D317/60

CPC分类号： C07D317/60

摘要： A process for preparing 3,4-methylenedioxymandelic acid by reacting 1,2-methylenedioxybenzene with glyoxylic acid in the presence of a strong acid, characterized in that the reaction is conducted in the presence of an aprotic organic solvent and 100 to 1200 ml of at least one member selected from the group consisting of organic acids per kg of 1,2-methylenedioxybenzene.

公开(公告)号：EP1352898A4

公开(公告)日：2005-07-20

申请号：EP01272314

申请日：2001-12-25

申请人： UBE INDUSTRIES

发明人： HARADA KATSUMASA ,  NISHINO SHIGEYOSHI ,  HIROTSU KENJI ,  NAKAMURA AKIRA ,  HARADA TAKASHI

IPC分类号： C07C253/30 ,  C07C255/17 ,  C07C255/31

CPC分类号： C07C253/30 ,  C07C2601/02 ,  C07C255/17 ,  C07C255/31

摘要： A process comprising reacting an aliphatic carboxylic ester compound with acetonitrile in the presence of a metal alkoxide to yield a metal salt of a β-ketonitrile compound, subsequently transferring the salt to an aqueous medium, and neutralizing the solution to obtain the β-Ketonitrile compound in a free state, wherein a water-incompatible organic solvent and water are added to the reaction mixture containing the β-Ketonotrile compound metal salt yielded to transfer the metal salt to the water, the resultant aqueous solution of the β-Ketonitrile compound metal salt is separated from the organic solvent by phase separation or another technique and then neutralized, and the resultant free β- Ketonitrile compound is taken out by extraction with an organic solvent.

摘要翻译： 在金属醇盐存在下，使脂肪族羧酸酯化合物与乙腈反应，生成β-酮腈化合物的金属盐后，将其转移到水性介质中，中和该溶液，得到β-酮腈化合物 在游离状态下，向含有β-酮化合物金属盐的反应混合物中加入水不相容有机溶剂和水，将所得金属盐转移到水中，得到的β-酮腈化合物金属盐水溶液 通过相分离或其他技术从有机溶剂中分离出来，然后中和，并且通过用有机溶剂萃取而将所得的游离β-乙腈化合物取出。

公开(公告)号：EP1247807A4

公开(公告)日：2003-02-12

申请号：EP00980002

申请日：2000-12-08

申请人： UBE INDUSTRIES

发明人： HARADA KATSUMASA ,  NISHINO SHIGEYOSHI ,  SHIMA HIDETAKA ,  NISHIMURA MINORU ,  HIROTSU KENJI

IPC分类号： C07D309/08 ,  C07D309/14

CPC分类号： C07D309/14 ,  C07D309/08

摘要： A process for producing a tetrahydropyranyl-4-sulfonate characterized by reacting 3-buten-1-ol, which is easily available, with a formaldehyde compound and an organic sulfonic acid; and a process suitable for the industrial production of a 4-aminotetrahydropyran derivative, by which the derivative can be produced in high yield under mild conditions through a simple procedure.

摘要翻译： 一种制备四氢吡喃基-4-磺酸酯的方法，其特征在于使容易获得的3-丁烯-1-醇与甲醛化合物和有机磺酸反应; 以及适用于4-氨基四氢吡喃衍生物的工业生产的方法，通过该方法可以在温和条件下通过简单的程序高产率地制备衍生物。

公开(公告)号：EP1367047A4

公开(公告)日：2005-12-07

申请号：EP02703866

申请日：2002-02-21

申请人： UBE INDUSTRIES

发明人： HARADA KATSUMASA ,  FUKUDA YASUHISA ,  YAMANAKA YOSHINORI

IPC分类号： C07C249/12 ,  C07C251/44 ,  C07B61/00

CPC分类号： C07C249/12 ,  C07C2601/20 ,  C07C251/44

摘要： A process for producing a 2-halogenocycloalkanone oxime, characterized by reducing a 2-halogenocycloalkenone oxime compound with hydrogen in the presence of a catalyst containing a supported platinum metal.

摘要翻译： 一种生产2-卤代环烷酮肟的方法，其特征在于在含有负载铂金属的催化剂存在下用氢还原2-卤代环烯酮肟化合物。

公开(公告)号：EP1251123A4

公开(公告)日：2003-02-05

申请号：EP01901537

申请日：2001-01-24

申请人： UBE INDUSTRIES ,  NISSAN CHEMICAL IND LTD

发明人： HARADA KATSUMASA ,  NISHINO SHIGEYOSHI ,  OKADA NAOKO ,  SHIMA HIDETAKA ,  HARADA TAKASHI

IPC分类号： C07D215/12 ,  C07D215/14

CPC分类号： C07D215/12

摘要： 3-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]prop-2-enenitrile is prepared by reacting 2-cyclopropyl-4- (4-fluorophenyl)quinoline-3-carbaldehyde with acetonitrile in the presence of a base and then adding a dehydrating agent to the reaction mixture to conduct dehydration. Under ordinary conditions, novel 3-[2-cyclopropyl-4-(4-fluorophenyl)-quinolin-3-yl]-3-hydroxypropionitrile is formed as an intermediate in the above reaction. Incidentally, when the above reaction is conducted in an organic solvent, 3-[2- cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]prop-2-enenitrile is directly formed.

公开(公告)号：EP0922704A4

公开(公告)日：2002-01-02

申请号：EP97936857

申请日：1997-08-22

申请人： NIPPON CHEMIPHAR CO ,  UBE INDUSTRIES

发明人： YAMAMOTO MASAO ,  KOBAYASHI KUNIO ,  HARADA KATSUMASA ,  NISHINO SHIGEYOSHI ,  SASAKI HIROSHI

IPC分类号： C07D337/14 ,  C07C205/56 ,  C07C229/40 ,  C07C323/62 ,  C07C229/42 ,  C07C233/11 ,  C07C255/41

CPC分类号： C07D337/14

摘要： A novel process for preparing zaltoprofen[2-(10,11-dihydro-10-oxodibenzo[b,f]thiepin-2-yl)propionic acid], which, as compared with the conventional processes, has better practicality from an overall viewpoint including availability and handleability of a starting material and profitability, such as the yield. The novel process is characterized by providing 2-(4-amino-3-carboxymethylphenyl)propionic acid or a salt thereof as a starting compound, subjecting the starting compound to, e.g., diazotization reacting the diazotized compound with thiophenol to prepare 2-(3-carboxymethyl-4-phenylthiophenyl)propionic acid or a salt thereof, and then subjecting this product to a ring-closing reaction. Intermediate compounds useful for the preparation of the above compound are also provided.