公开(公告)号：JPS61267589A

公开(公告)日：1986-11-27

申请号：JP26062285

申请日：1985-11-20

申请人： SANKYO CO

发明人： HARASHIMA TATSU ,  ODA OSAMU

IPC分类号： C07D317/72 ,  C07B31/00 ,  C07B41/02 ,  C07C27/00 ,  C07C29/136 ,  C07C29/143 ,  C07C35/08 ,  C07C35/18 ,  C07C35/30 ,  C07C41/00 ,  C07C43/178 ,  C07C51/00 ,  C07C59/125 ,  C07C59/46 ,  C07C59/58 ,  C07C67/00 ,  C07C313/00 ,  C07C323/15 ,  C07C401/00 ,  C07C405/00 ,  C07D309/00 ,  C07D309/06 ,  C07D317/00 ,  C07D339/06 ,  C07D407/04 ,  C07D407/12 ,  C07F5/06 ,  C07F7/18

摘要： NEW MATERIAL:A compound shown by the formula I (M is alkali metal; R is alkyl; R is alkyl which may be replaced with halogen or aryl which may be replaced with halogen, trihalogenomethyl or alkyl). EXAMPLE:Sodium hydride bis(2-methoxyethoxy)(hexafluoroisopropoxy)aluminum. USE:A reducing agent especially useful for reducing carbonyl group to give stereospecific hydroxyl group, for example, it is used for reducing carbonyl group at the 15-position in prostaglandin synthesis. PREPARATION:A compound shown by the formula II is reacted with a compound shown by the formula R -OH in a ratio of the latter to the former of usually 0.5-1.5mol to 1mol preferably in a solvent approximately at 0 deg.C.

公开(公告)号：JP2002275141A

公开(公告)日：2002-09-25

申请号：JP2001393530

申请日：2001-12-26

申请人： SANKYO CO

发明人： OYAMA YUZURU ,  TANABE HIDEO ,  HARASHIMA TATSU

IPC分类号： C07D277/14 ,  C07B43/06 ,  C07B61/00 ,  C07C231/02 ,  C07C233/13

摘要： PROBLEM TO BE SOLVED: To provide a method for producing a desired carboxylic acid amide in a good yield by reacting a carboxylic acid compound with an amino compound. SOLUTION: This method for producing a carboxylic acid amide comprises reacting a carboxylic acid with an amino compound in the presence of an alkanephosphonic anhydride and an N-alkylimidazole.

公开(公告)号：JPH0576952B2

公开(公告)日：1993-10-25

申请号：JP26062285

申请日：1985-11-20

申请人： SANKYO CO

发明人： HARASHIMA TATSU ,  ODA OSAMU

IPC分类号： C07D317/72 ,  C07B31/00 ,  C07B41/02 ,  C07C27/00 ,  C07C29/136 ,  C07C29/143 ,  C07C35/08 ,  C07C35/18 ,  C07C35/30 ,  C07C41/00 ,  C07C43/178 ,  C07C51/00 ,  C07C59/125 ,  C07C59/46 ,  C07C59/58 ,  C07C67/00 ,  C07C313/00 ,  C07C323/15 ,  C07C401/00 ,  C07C405/00 ,  C07D309/00 ,  C07D309/06 ,  C07D317/00 ,  C07D339/06 ,  C07D407/04 ,  C07D407/12 ,  C07F5/06 ,  C07F7/18

公开(公告)号：JP2006008699A

公开(公告)日：2006-01-12

申请号：JP2005230800

申请日：2005-08-09

申请人： Sankyo Co Ltd ,  三共株式会社

发明人： TAKITA TAKASHI ,  OTSUKA KEIICHI ,  NUMAGAMI EIJI ,  HARASHIMA TATSU

IPC分类号： A61K31/7068 ,  A61P35/00 ,  C07D405/04 ,  C07H19/06

CPC分类号： C07H19/06

摘要： PROBLEM TO BE SOLVED: To provide the crystals of a pyrimidine nucleoside derivative having an excellent anti-tumor activity.
SOLUTION: This medicine contains the crystals of the compound represented by formula (I) or its hydrate as an active ingredient. Since the crystals of the compound represented by formula (I) have remarkably improved storage stability and handling easiness as compared to the powder of the compound, and are excellent in actions in bodies, such as oral absorbability, the crystals of the compound are extremely useful on practical uses as the medicine.
COPYRIGHT: (C)2006,JPO&NCIPI

摘要翻译： 待解决的问题：提供具有优异抗肿瘤活性的嘧啶核苷衍生物的晶体。 解决方案：该药含有由式（I）表示的化合物或其水合物作为活性成分的晶体。 由于式（I）表示的化合物的晶体与化合物的粉末相比具有显着提高的储存稳定性和处理容易性，并且在体内的作用如口服吸收性方面优异，所以化合物的晶体是非常有用的 以实用为药。 版权所有（C）2006，JPO＆NCIPI

公开(公告)号：JP2002308895A

公开(公告)日：2002-10-23

申请号：JP2002026232

申请日：2002-02-04

申请人： SANKYO CO

发明人： TAKITA TAKASHI ,  OTSUKA KEIICHI ,  NUMAGAMI EIJI ,  HARASHIMA TATSU

IPC分类号： A61K31/7068 ,  A61P35/00 ,  C07D405/04 ,  C07H19/06

摘要： PROBLEM TO BE SOLVED: To provide a crystal of a pyrimidine nucleoside derivative having an excellent antitumor activity. SOLUTION: The crystal of the compound is represented by formula (I).

公开(公告)号：JPH0625215A

公开(公告)日：1994-02-01

申请号：JP10240893

申请日：1993-04-28

申请人： SANKYO CO

发明人： HARASHIMA TATSU ,  ODA OSAMU

IPC分类号： C07D317/72 ,  C07B31/00 ,  C07B41/02 ,  C07C27/00 ,  C07C29/136 ,  C07C29/143 ,  C07C35/08 ,  C07C35/18 ,  C07C35/30 ,  C07C41/00 ,  C07C43/178 ,  C07C51/00 ,  C07C59/125 ,  C07C59/46 ,  C07C59/58 ,  C07C67/00 ,  C07C313/00 ,  C07C323/15 ,  C07C401/00 ,  C07C405/00 ,  C07D309/00 ,  C07D309/06 ,  C07D317/00 ,  C07D339/06 ,  C07D407/04 ,  C07D407/12 ,  C07F5/06 ,  C07F7/18

摘要： PURPOSE:To advantageously produce a stereospecific hydroxyl groupcontaining compound by reducing a carbonyl group of a carbonyl group-containing compound by using a specific reducing agent having stereospecificity. CONSTITUTION:In obtaining a compound of formula III (e.g. compound of formula IV) by reducing a compound of formula I [R is OH-protecting group; R is alkyl, alkenyl, aryl, etc.; X is group of formula II (Y is carbonyl-protecting group), etc.], a reducing agent having stereospecificity is used. A compound of formula V [M is Na or Li; R is alkyl; R is alkyl or phenyl (may be replaced with halogen, trihalogenomethyl or alkyl)], especially a compound wherein M is Na, R is methyl or ethyl and R is ethyl, n-propyl, 2-fluoroethyl, phenyl, naphthyl, etc., is preferable as the reducing agent. This reducing agent of formula V is obtained by bringing a compound of formula VI into contact with a compound of formula VII.