CN106518778A - Synthetic method for pharmaceutical intermediate namely 2-ethyl-5-fluoro-6-bromopyrimidine-4-ketone - Google Patents
Synthetic method for pharmaceutical intermediate namely 2-ethyl-5-fluoro-6-bromopyrimidine-4-ketone Download PDFInfo
- Publication number
- CN106518778A CN106518778A CN201610910052.1A CN201610910052A CN106518778A CN 106518778 A CN106518778 A CN 106518778A CN 201610910052 A CN201610910052 A CN 201610910052A CN 106518778 A CN106518778 A CN 106518778A
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- CN
- China
- Prior art keywords
- fluoro
- ketone
- ethyl
- synthetic method
- bromopyrimidine
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- 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.)
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/34—One oxygen atom
- C07D239/36—One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention relates to a synthetic method for a pharmaceutical intermediate namely 2-ethyl-5-fluoro-6-bromopyrimidine-4-ketone. The synthetic method synthesizes 2-ethyl-5-fluoro-6-bromopyrimidine-4-ketone with 5-fluoro-6-chloropyrimidine-4-ketone as a raw material successively through ethylation and bromine replacement reactions under the actions of a diethyl ether solvent and 1.5 atmospheres at a temperature of 120 DEG C to 160 DEG C. The synthetic method for the pharmaceutical intermediate namely 2-ethyl-5-fluoro-6-bromopyrimidine-4-ketone provided by the invention has the advantages of simplicity, high efficiency, safe operation, and significant practicality in concrete production.
Description
Technical field
The present invention relates to a kind of synthetic method of the fluoro- 6- Bromopyrimidines -4- ketone of medicine intermediate 2- ethyl -5-.
Background technology
The synthetic method of the fluoro- 6- Bromopyrimidines -4- ketone of 2- ethyl -5- is the initiation material of many pharmaceutical synthesis, particularly very
The important intermediate of many pyrimidinone compounds, the current country have no the synthetic method for reporting this compound.
The content of the invention
It is an object of the invention to overcome above-mentioned deficiency, there is provided a kind of simple, efficient, medicine intermediate 2- of safety operation
The synthetic method of the fluoro- 6- Bromopyrimidines -4- ketone of ethyl -5-.
The object of the present invention is achieved like this：
A kind of synthetic method of the fluoro- 6- Bromopyrimidines -4- ketone of medicine intermediate 2- ethyl -5-, with the fluoro- 6- chlorine pyrimidin-4-ones of 5- be
Raw material, in the presence of solvent ether and 1.5 atmospheric pressure, at 120 DEG C -160 DEG C of temperature, is successively put by ethylization and bromine
Reaction is changed, the synthetic method of the fluoro- 6- Bromopyrimidines -4- ketone of 2- ethyl -5- is generated.
Compared with prior art, the invention has the beneficial effects as follows：
The synthetic method of the fluoro- 6- Bromopyrimidines -4- ketone of medicine intermediate 2- ethyl -5- of the present invention is simple, efficiently, and operate peace
Entirely, it is very useful in concrete production.
Specific embodiment
The synthetic method of the fluoro- 6- Bromopyrimidines -4- ketone of medicine intermediate 2- ethyl -5- of the present invention is specific as follows：
With the fluoro- 6- chlorine pyrimidin-4-ones of 5- as raw material, in the presence of solvent ether and 1.5 atmospheric pressure, 120 DEG C of temperature-
At 160 DEG C, successively by ethylizing and bromine displacement reaction, the synthetic method of the fluoro- 6- Bromopyrimidines -4- ketone of 2- ethyl -5- is generated.This
The purity of crude product can meet general reaction requirement, can direct plunge in reaction.
Claims (1)
1. the synthetic method of the fluoro- 6- Bromopyrimidines -4- ketone of a kind of medicine intermediate 2- ethyl -5-, it is characterised in that with the fluoro- 6- chlorine of 5-
Pyrimidin-4-one is raw material, in the presence of solvent ether and 1.5 atmospheric pressure, at 120 DEG C -160 DEG C of temperature, is successively passed through
Ethylize and bromine displacement reaction, generate the synthetic method of the fluoro- 6- Bromopyrimidines -4- ketone of 2- ethyl -5-.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610910052.1A CN106518778A (en) | 2016-10-19 | 2016-10-19 | Synthetic method for pharmaceutical intermediate namely 2-ethyl-5-fluoro-6-bromopyrimidine-4-ketone |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610910052.1A CN106518778A (en) | 2016-10-19 | 2016-10-19 | Synthetic method for pharmaceutical intermediate namely 2-ethyl-5-fluoro-6-bromopyrimidine-4-ketone |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106518778A true CN106518778A (en) | 2017-03-22 |
Family
ID=58332536
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610910052.1A Pending CN106518778A (en) | 2016-10-19 | 2016-10-19 | Synthetic method for pharmaceutical intermediate namely 2-ethyl-5-fluoro-6-bromopyrimidine-4-ketone |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN106518778A (en) |
-
2016
- 2016-10-19 CN CN201610910052.1A patent/CN106518778A/en active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20170322 |