JPS5732270A - Preparation of 3-substituted-5-halogenated uracil - Google Patents

Preparation of 3-substituted-5-halogenated uracil

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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
Application number
JP10799580A
Other languages
Japanese (ja)
Inventor
Wataru Nagata
Susumu Kamata
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shionogi and Co Ltd
Original Assignee
Shionogi and Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Shionogi and Co Ltd filed Critical Shionogi and Co Ltd
Priority to JP10799580A priority Critical patent/JPS5732270A/en
Publication of JPS5732270A publication Critical patent/JPS5732270A/en
Pending legal-status Critical Current

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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
JP10799580A 1980-08-05 1980-08-05 Preparation of 3-substituted-5-halogenated uracil Pending JPS5732270A (en)

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)

* Cited by examiner, † Cited by third party
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

Cited By (2)

* Cited by examiner, † Cited by third party
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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