JPS5695173A - Preparation of 5-fluorocytosine - Google Patents
Preparation of 5-fluorocytosineInfo
- Publication number
- JPS5695173A JPS5695173A JP17159779A JP17159779A JPS5695173A JP S5695173 A JPS5695173 A JP S5695173A JP 17159779 A JP17159779 A JP 17159779A JP 17159779 A JP17159779 A JP 17159779A JP S5695173 A JPS5695173 A JP S5695173A
- Authority
- JP
- Japan
- Prior art keywords
- hydrogen fluoride
- cytosine
- fluorine
- reaction
- amino group
- 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.)
- Granted
Links
Abstract
PURPOSE:The obtain the titled compound useful as an intermediate for an agent for candidiasis, carcinostatic, etc. industrially advantageously, by reacting cytosine with fluorine in the presence of hydrogen fluoride in an amount sufficient for the proceeding of the reaction at a temperature not causing release of amino group at 4-position. CONSTITUTION:In the presence of hydrogen fluoride, cytosine is reacted with fluorine at a temperature (at about not higher than 40 deg.C) not causing deamination of amino group at 4-position. After the separation of the intermediate, after treatment is carried out, for example, by adding water and a methanol solvent to the reaction product to elute excess hydrogen fluoride, treating it with a tertiary amine to dehydrate, followed by deacidification to give the desired compound. Hydrogen fluoride is used alone, or may be used in the presence of water, halogenated hydrocarbon, ketone, organic acid, alcohol, etc. in an amount not to inhibit the reaction as a coexisting solvent. Fluorine gas in a molar ratio of it to cytosine of 1.0-2.0: 1 is necessary, and preferably diluted with an inert gas for use.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP17159779A JPS5695173A (en) | 1979-12-28 | 1979-12-28 | Preparation of 5-fluorocytosine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP17159779A JPS5695173A (en) | 1979-12-28 | 1979-12-28 | Preparation of 5-fluorocytosine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS5695173A true JPS5695173A (en) | 1981-08-01 |
| JPS6252749B2 JPS6252749B2 (en) | 1987-11-06 |
Family
ID=15926108
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP17159779A Granted JPS5695173A (en) | 1979-12-28 | 1979-12-28 | Preparation of 5-fluorocytosine |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS5695173A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106554115A (en) * | 2016-12-08 | 2017-04-05 | 西安润格环保科技有限公司 | A kind of coal chemical industrial waste water is reduced pressure depickling deamination method and system step by step |
| CN110615767A (en) * | 2019-10-26 | 2019-12-27 | 新乡拓新药业股份有限公司 | Method for synthesizing 5-fluorocytosine |
| CN110746360A (en) * | 2019-10-26 | 2020-02-04 | 新乡拓新药业股份有限公司 | Method for synthesizing 5-fluorocytosine |
| US10995075B2 (en) | 2014-08-29 | 2021-05-04 | University Of Durham | Process for producing fluorocytosine and fluorocytosine derivatives |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH01305259A (en) * | 1988-06-03 | 1989-12-08 | Matsushita Electric Ind Co Ltd | Hot water supplying apparatus |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS4976882A (en) * | 1972-11-28 | 1974-07-24 |
-
1979
- 1979-12-28 JP JP17159779A patent/JPS5695173A/en active Granted
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS4976882A (en) * | 1972-11-28 | 1974-07-24 |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10995075B2 (en) | 2014-08-29 | 2021-05-04 | University Of Durham | Process for producing fluorocytosine and fluorocytosine derivatives |
| CN106554115A (en) * | 2016-12-08 | 2017-04-05 | 西安润格环保科技有限公司 | A kind of coal chemical industrial waste water is reduced pressure depickling deamination method and system step by step |
| CN110615767A (en) * | 2019-10-26 | 2019-12-27 | 新乡拓新药业股份有限公司 | Method for synthesizing 5-fluorocytosine |
| CN110746360A (en) * | 2019-10-26 | 2020-02-04 | 新乡拓新药业股份有限公司 | Method for synthesizing 5-fluorocytosine |
| CN110615767B (en) * | 2019-10-26 | 2022-06-28 | 新乡拓新药业股份有限公司 | Method for synthesizing 5-fluorocytosine |
| CN110746360B (en) * | 2019-10-26 | 2022-06-28 | 新乡拓新药业股份有限公司 | Method for synthesizing 5-fluorocytosine |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS6252749B2 (en) | 1987-11-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| LAPS | Cancellation because of no payment of annual fees |