公开(公告)号：EP1176150A1

公开(公告)日：2002-01-30

申请号：EP01902834.9

申请日：2001-02-09

申请人： Mitsui Chemicals, Inc.

发明人： UMETANI, Hideki ,  FUKAZAWA, Nobuyuki ,  KOMATSU, Hironori

IPC分类号： C07H19/073

CPC分类号： C07H19/06

摘要： 5-trifluoromethyl-2,4-bis(trimethylsilyloxy)pyrimidi ne is reacted with a 2-deoxy-α-D-erythro-pentofuranosyl chloride derivative reacted in the absence or presence of a small amount of solvent to give a β-form of 1-(2'-deoxy-β-D-erythro-pentofuranosyl)-5-trifluoromethyl uracil derivative with a high selectivity.

摘要翻译： 5-三氟甲基-2,4-双（三甲基甲硅烷氧基）嘧啶与在不存在或存在少量溶剂的情况下反应的2-脱氧-α-D-赤型 - 戊呋喃糖基氯衍生物反应，得到β- 1-（2'-脱氧-β-D-赤 - 戊呋喃糖基）-5-三氟甲基尿嘧啶衍生物。

公开(公告)号：EP0603404B1

公开(公告)日：1999-03-17

申请号：EP93910331.3

申请日：1993-05-13

申请人： MITSUI CHEMICALS, INC.

发明人： FUKAZAWA, Nobuyuki ,  SUZUKI, Tsuneji ,  KAWAUCHI, Nobuya ,  KOMATSU, Hironori ,  OTSUKA, Kengo ,  NAKAJIMA, Yuki

IPC分类号： C07D301/00 ,  C07D303/23 ,  C07D405/12 ,  C07D303/22

CPC分类号： C07D303/22 ,  C07D405/12

摘要： A process for producing a glycide derivative represented by general formula (I), which comprises reacting an aryl or heteroaryl alcohol represented by A-OH with glycidyl tosylate in the presence of a cesium base. In formula (I) A represents aryl or heteroaryl. This process enables an aryl glycidyl ether derivative, an important intermediate for the production of medicines, to be produced readily without fail and can provide a compound with a high optical purity particularly when optically active glycidyl tosylate is used.

公开(公告)号：EP1176150B1

公开(公告)日：2005-10-19

申请号：EP01902834.9

申请日：2001-02-09

申请人： Mitsui Chemicals, Inc.

发明人： UMETANI, Hideki ,  FUKAZAWA, Nobuyuki ,  KOMATSU, Hironori

IPC分类号： C07H19/073

CPC分类号： C07H19/06

摘要： 5-trifluoromethyl-2,4-bis(trimethylsilyloxy)pyrimidi ne is reacted with a 2-deoxy- alpha -D-erythro-pentofuranosyl chloride derivative reacted in the absence or presence of a small amount of solvent to give a beta -form of 1-(2'-deoxy- beta -D-erythro-pentofuranosyl)-5-trifluoromethyl uracil derivative with a high selectivity.

公开(公告)号：EP1178051A2

公开(公告)日：2002-02-06

申请号：EP01904386.8

申请日：2001-02-13

申请人： Mitsui Chemicals, Inc.

发明人： KOMATSU, Hironori ,  AWANO, Hirokazu ,  FUKAZAWA, Nobuyuki ,  ITO, Kiyoshi ,  IKEDA, Ichirou ,  ARAKI, Tadashi ,  NAKAMURA, Takeshi ,  ASANO, Tamotsu ,  FUJIWARA, Junya ,  ANDO, Tomoyuki ,  TSUCHIYA, Katsutoshi ,  MARUYAMA, Kyoko ,  UMETANI, Hideki ,  YAMAUCHI, Takahiro ,  MIYAKE, Hitoki

IPC分类号： C07F9/655 ,  C07H1/02 ,  C07H19/20 ,  C07H19/12 ,  C07H19/19 ,  C07H19/23 ,  C07H13/08 ,  C07H11/04 ,  C12P19/38

CPC分类号： C07H19/10 ,  C07H19/00 ,  C07H19/20

摘要： A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.

摘要翻译： 期望的异构体通过选择性phosphorolyzing和异构化1磷酸化衍生物的端基异构体混合物的糖类而结晶化的异构体中的一个来置换平衡制备。 进一步，使用核苷磷酸化酶的作用下，一个核苷从得到的1-磷酸化糖衍生物和具有改进的立体选择性碱和更高的产率制备。 该过程用于制备1-磷酸化糖衍生物和核苷端基异构体的选择性过程。

公开(公告)号：EP1178051B1

公开(公告)日：2008-05-28

申请号：EP01904386.8

申请日：2001-02-13

申请人： Mitsui Chemicals, Inc.

发明人： KOMATSU, Hironori ,  AWANO, Hirokazu ,  FUKAZAWA, Nobuyuki ,  ITO, Kiyoshi ,  IKEDA, Ichirou ,  ARAKI, Tadashi ,  NAKAMURA, Takeshi ,  ASANO, Tamotsu ,  FUJIWARA, Junya ,  ANDO, Tomoyuki ,  TSUCHIYA, Katsutoshi ,  MARUYAMA, Kyoko ,  UMETANI, Hideki ,  YAMAUCHI, Takahiro ,  MIYAKE, Hitoki

IPC分类号： C07F9/655 ,  C07H1/02 ,  C07H19/20 ,  C07H19/12 ,  C07H19/19 ,  C07H19/23 ,  C07H13/08 ,  C07H11/04 ,  C12P19/38 ,  C07H1/04

CPC分类号： C07H19/10 ,  C07H19/00 ,  C07H19/20

摘要： A mixture of 1-phosphorylated sugar derivative anomers is phosphorolyzed and isomerized to thereby crystallize one of the anomers. Thus, the equilibrium is shifted and a desired isomer alone is selectively produced. From the 1-phosphorylated sugar derivative thus obtained and a base, a nucleoside is produced at a high stereoselectivity and a high yield under the action of a nucleoside phosphorylase. Thus, a process for anomer-selectively producing a 1-phosphorylated sugar derivative and a process for producing a nucleoside are provided.

公开(公告)号：EP0711768B1

公开(公告)日：2002-02-13

申请号：EP95919662.7

申请日：1995-05-30

申请人： MITSUI CHEMICALS, INC.

发明人： MATSUNAGA, Akio ,  NAKAJIMA, Yuki ,  KOHNO, Hiroshi ,  KOMATSU, Hironori ,  EDATSUGI, Hajime ,  IWATA, Daiji ,  TAKEZAWA, Kimiko

IPC分类号： C07D403/04 ,  C07D409/04 ,  C07D405/04 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D407/14 ,  A61K31/44 ,  A61K31/415 ,  A61K31/535

CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04

摘要： A novel compound represented by general formula (1) or a pharmacologically acceptable salt thereof, being useful as anticancer, antiviral and antibacterial agents.