JPS5732270A - Preparation of 3-substituted-5-halogenated uracil - Google Patents
Preparation of 3-substituted-5-halogenated uracilInfo
- Publication number
- JPS5732270A JPS5732270A JP10799580A JP10799580A JPS5732270A JP S5732270 A JPS5732270 A JP S5732270A JP 10799580 A JP10799580 A JP 10799580A JP 10799580 A JP10799580 A JP 10799580A JP S5732270 A JPS5732270 A JP S5732270A
- Authority
- JP
- Japan
- Prior art keywords
- formula
- compound
- halogen
- reacting
- product
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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- Plural Heterocyclic Compounds (AREA)
Abstract
PURPOSE: To prepare the titled compound, easily, in high yield, by reacting a 5- halogenated uracil with an acrylating agent, reacting the product with a compound such as alkyl halide, and finally removing the 1-position carboxy ester group from the reaction product.
CONSTITUTION: Condensation of the 5-halogenated uracil of formula I (X is halogen, esp. F) with an acylating agent of formula II (R1 is alkyl or aralkyl; Y1 is halogen) to obtain the 1-carboxyl ester compond of formula III, which is condensed with the compound of formula IV (R is R1, trialkylsilyloxyalkoxyalkyl, tetrahydrofuryl, 5-oxo-2,3,4,5-tetrahydro-2-furyl, etc.; Y2 is Y1). The objective compound of formula VI can be prepared by removing the 1-position carboxy ester group of the condensation product of formula V, e.g. by hydrolysis with an alkali.
EFFECT: Toxicity, etc. of an antitumor agent, 5-fluorouracil, can be improved.
COPYRIGHT: (C)1982,JPO&Japio
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP10799580A JPS5732270A (en) | 1980-08-05 | 1980-08-05 | Preparation of 3-substituted-5-halogenated uracil |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP10799580A JPS5732270A (en) | 1980-08-05 | 1980-08-05 | Preparation of 3-substituted-5-halogenated uracil |
Publications (1)
Publication Number | Publication Date |
---|---|
JPS5732270A true JPS5732270A (en) | 1982-02-20 |
Family
ID=14473309
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP10799580A Pending JPS5732270A (en) | 1980-08-05 | 1980-08-05 | Preparation of 3-substituted-5-halogenated uracil |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPS5732270A (en) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4528372A (en) * | 1980-10-09 | 1985-07-09 | Grelan Pharmaceutical Co., Ltd. | N-Phthalidyl-5-fluorouracils |
US4605738A (en) * | 1982-11-18 | 1986-08-12 | Shionogi & Co., Ltd. | Production of 1-phthalidyl-5-fluorouracil derivatives |
-
1980
- 1980-08-05 JP JP10799580A patent/JPS5732270A/en active Pending
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4528372A (en) * | 1980-10-09 | 1985-07-09 | Grelan Pharmaceutical Co., Ltd. | N-Phthalidyl-5-fluorouracils |
US4605738A (en) * | 1982-11-18 | 1986-08-12 | Shionogi & Co., Ltd. | Production of 1-phthalidyl-5-fluorouracil derivatives |
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