公开(公告)号：CA2017678A1

公开(公告)日：1990-11-30

申请号：CA2017678

申请日：1990-05-28

Applicant: UBE INDUSTRIES

Inventor： KODA AKIHIDE ,  KITA JUN ICHIRO ,  KAKU YOSHIO ,  HORIMI IICHIRO ,  SAKAMOTO OSAMI

IPC: C07D239/54 ,  C07D239/553 ,  C07H19/06 ,  C07H19/067 ,  A61K31/505 ,  A61K31/70

Abstract: : 5-Fluorouracil derivative There are diclosed a 5-fluorouracil derivative represented by the formula (1): (1) wherein A represents a group represented by or wherein R1 represents a hydrogen atom or OR5 group, R2, R3 and R5 may be the same or different and each represents a hydrogen atom or a group represented by the following formula (2): (2) wherein R6 represents an acyl group, R7 represents a hydrogen atom, a straight or branched alkyl group, a cycloalkyl group, an aralkyl group, a lower alkenyl group or a phenyl group, and n is an integer of 0 to 6, provided that at least one of R2, R3 and R5 is a group represented by the formula (2), and the case wherein R2 and R5 are both hydrogen atoms is excluded, R4 represents a group represented by the formula (2), and X represents an alkylene group or a cycloalkylene group, and an antitumor agent containing the same as an active ingredient.

公开(公告)号：JPH032193A

公开(公告)日：1991-01-08

申请号：JP13480689

申请日：1989-05-30

Applicant: UBE INDUSTRIES

Inventor： EDA SHOEI ,  KITA JUNICHIRO ,  KAKU YOSHIO ,  SAKAMOTO OSAMI

IPC: C07H19/067 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7072 ,  A61P35/00 ,  C07H19/073

Abstract: NEW MATERIAL:A compound of formula I {R is H or OR ; R to R are each H or of formula II [R is acyl; R is H, 1-13C alkyl, cycloalkyl, aralkyl, (halogen-substituted) lower alkenyl or (substituted)phenyl; n is 0-6], where, at least one of R to R being of formula II and R and R are not H at the same time.} EXAMPLE:2',3',5'-tris-O-[N-(2-n-propyl-n-pentanoyl)glycyl]-5-fluorouri dine. USE:Antineoplastic agents. Low toxic. PREPARATION:A 5-fluorouridine of formula III (R is H or OH) or 2'-deoxy-5- fluorouridine is put to ester condensation with a compound of formula IV in a solvent such as dichloromethane in the presence of a base such as a trialkylamine and a condensation agent such as p-toluenesulfonyl chloride.