Patent US3846429A successfully refreshed from Google Patents.
US3846429A
Expired / Lapsed
US
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Method of producing 5-fluorouracil
Assignee: Individual
•
Filing: 1971-09-22
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Granted: 1974-11-05
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Expires: 1991-09-22
Abstract
Abstract A method of producing 5-fluorouracil which includes the fluorination of uracil with elementary fluorine diluted with an inert gas in a glacial acetic acid medium under hydrodynamic conditions of Re 35,000-45,000 at a temperature of from 15* to 35* until the uracil disappears from the reaction mixture, whereafter said mixture is heated at a temperature of from 90* to 95*C until 5-fluoro-6-acetoxy-dihydrouracil formed during the fluorination disappears therefrom, followed by isolation of the desired product. The 5-fluorouracil compound is useful as a chemotherapeutical remedy for treating cancer of the alimentary tract and also as a starting material for synthesizing other antitumoric substances.
Inventors
- 👤 D Sniker
- 👤 I Knunyants
- 👤 L German
- 👤 N Kazmina
- 👤 A Lazdinsh
- 👤 A Veinberg
- 👤 S Giller
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 16:49
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/52; C07D239/54
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
70 words
A METHOD OF PRODUCING 5-FLUOROURACIL COMPRISING THE STEPS OF FLUORINATING URACIL WITH ELEMENTARY FLUORINE DILUTED WITH AN INERT GAS IN A GLACIAL ACETIC ACID MEDIUM UNDER HYDRODYNAMIC CONDITIONS OF RE=35,000-45,000 AT A TEMPERATURE OF FROM 15* TO 35*C UNTIL THE URACIL DISAPPEARS FROM THE REACTION MIXTURE, HEATING SAID MIXTURE AT A TEMPERATURE OF FROM 90* TO 95*C UNTIL 5-FLUORO-6-ACETOXY-DIHYDROURACIL FORMED DURING THE FLUORINATION DISAPPEARS THEREFROM AND ISOLATING THE DESIRED PRODUCT.
Claim 2
Independent Claim
70 words
A METHOD OF PRODUCING 5-FLUOROURACIL COMPRISING THE STEPS OF FLUORINATING URACIL WITH ELEMENTARY FLUORINE DILUTED WITH AN INERT GAS IN A GLACIAL ACETIC ACID MEDIUM UNDER HYDRODYNAMIC CONDITIONS OF RE=35,000-45,000 AT A TEMPERATURE OF FROM 15* TO 35*C UNTIL THE URACIL DISAPPEARS FROM THE REACTION MIXTURE, HEATING SAID MIXTURE AT A TEMPERATURE OF FROM 90* TO 95*C UNTIL 5-FLUORO-6-ACETOXY-DIHYDROURACIL FORMED DURING THE FLUORINATION DISAPPEARS THEREFROM AND ISOLATING THE DESIRED PRODUCT.
Claim 3
Dependent Claim
27 words
A method as claimed in claim 1, wherein uracil is employed for the reaction in an amount of 7-8 g. per 100 ml. of glacial acetic acid.
Claim 4
Dependent Claim
15 words
A method as claimed in claim 1, wherein nitrogen is employed as the inert gas.
Claim 5
Dependent Claim
20 words
A method as claimed in claim 1, wherein elementary fluorine is diluted with nitrogen at a volumetric ratio of 1:2.0-2.5.
Claim 6
Dependent Claim
55 words
A method as claimed in claim 1, wherein the reaction is effected at a rate of the gas mixture supply of 1.2-1.5 1/hr. per 1 g. of uracil until fluorine is traced in the offgases and then at a rate of 0.15-0.18 1/hr. per gram of uracil until the uracil disappears from the reaction mixture.
References Cited (Backward Citations)
US3682917A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1977-11-04 | 1978-05-06 | 1978-11-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1981-11-04 | 1982-05-06 | 1982-11-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1985-11-04 | 1986-05-06 | 1986-11-05 | $7700.00 | Window Closed / Lapsed |