CN104744371A - Preparation method of butoconazole - Google Patents
Preparation method of butoconazole Download PDFInfo
- Publication number
- CN104744371A CN104744371A CN201310727011.5A CN201310727011A CN104744371A CN 104744371 A CN104744371 A CN 104744371A CN 201310727011 A CN201310727011 A CN 201310727011A CN 104744371 A CN104744371 A CN 104744371A
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- China
- Prior art keywords
- butoconazole
- preparation
- chloro
- chlorine
- introduce
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
- C07D233/60—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
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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 preparation method of butoconazole. The method comprises the following specific steps: converting a raw material p-chlorobenzyl chloride into a Grignard reagent, reacting with chloro epoxypropane to obtain 1-4-chloro-p-chlorophenyl butanol-2, introducing imidazole, converting the hydroxyl into chlorine, introducing 2,6-dichloro thiophenol to obtain butoconazole, and acidifying with nitric acid to obtain butoconazole nitrate. The preparation method of butoconazole is simple in manufacture and low in production cost, and the butoconazole is an antifungal drug highly effective in the infection of Candida albicans and Candida albicans.
Description
Technical field
The present invention relates to the field that medicine manufactures, especially a kind of preparation method of butoconazole.
Background technology
Butoconazole is imidazoles antifungal drug, is mainly used in treating cloudy vaginal candidiasis, and butoconazole is white to off-white color crystalline powder, is slightly soluble in methyl alcohol, be slightly soluble in chloroform, methylene dichloride, acetone, ethanol, atomicly be dissolved in ethyl acetate, water-soluble hardly, fusing point about 159 °.Owing to being to produce butoconazole at present, manufacture complicated, production cost is high.
Summary of the invention
The technical problem to be solved in the present invention is: in order to overcome above-mentioned middle Problems existing, provide a kind of preparation method of butoconazole.
The technical solution adopted for the present invention to solve the technical problems is: a kind of preparation method of butoconazole, concrete steps are as follows: with p-chlorobenzyl chlorine for raw material, after being converted into Grignard reagent, and polychlorinated dibenzo-furans reaction, obtain 1-chloro-4-rubigan butanols-2, introduce imidazolyl, after again conversion of hydroxyl being chlorine, introduce 2,6-thiophenol dichlorobenzene, obtain butoconazole, can Butoconazole nitrate be obtained with nitric acid acidifying.
The invention has the beneficial effects as follows: the preparation method of described a kind of butoconazole, it manufactures simple, and production cost is low, is imidazoles antifungal drug, has efficient to Candida albicans, Oidium tropicale infection.
Embodiment
Be described in further detail in conjunction with the present invention now.
The preparation method of a kind of butoconazole of the present invention, concrete steps are as follows: with p-chlorobenzyl chlorine for raw material, after being converted into Grignard reagent, and polychlorinated dibenzo-furans reaction, obtain 1-chloro-4-rubigan butanols-2, introduce imidazolyl, after again conversion of hydroxyl being chlorine, introduce 2,6-thiophenol dichlorobenzene, obtain butoconazole, can Butoconazole nitrate be obtained with nitric acid acidifying.
With above-mentioned according to desirable embodiment of the present invention for enlightenment, by above-mentioned description, relevant staff in the scope not departing from this invention technological thought, can carry out various change and amendment completely.The technical scope of this invention is not limited to the content on specification sheets, must determine its technical scope according to right.
Claims (1)
1. the preparation method of a butoconazole, it is characterized in that concrete steps are as follows: with p-chlorobenzyl chlorine for raw material, after being converted into Grignard reagent, and polychlorinated dibenzo-furans reaction, obtain 1-chloro-4-rubigan butanols-2, introduce imidazolyl, after again conversion of hydroxyl being chlorine, introduce 2,6-thiophenol dichlorobenzene, obtain butoconazole, can Butoconazole nitrate be obtained with nitric acid acidifying.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310727011.5A CN104744371A (en) | 2013-12-25 | 2013-12-25 | Preparation method of butoconazole |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310727011.5A CN104744371A (en) | 2013-12-25 | 2013-12-25 | Preparation method of butoconazole |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN104744371A true CN104744371A (en) | 2015-07-01 |
Family
ID=53584720
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310727011.5A Pending CN104744371A (en) | 2013-12-25 | 2013-12-25 | Preparation method of butoconazole |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN104744371A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105218456A (en) * | 2015-10-09 | 2016-01-06 | 株洲千金药业股份有限公司 | A kind of method of suitability for industrialized production Nitric acid butoconazole |
| CN105218455A (en) * | 2015-10-09 | 2016-01-06 | 株洲千金药业股份有限公司 | A kind of method of industrialization continuous seepage Nitric acid butoconazole |
| CN105384600A (en) * | 2015-10-09 | 2016-03-09 | 株洲千金药业股份有限公司 | Industrial production method for butoconazole nitrate intermediate |
-
2013
- 2013-12-25 CN CN201310727011.5A patent/CN104744371A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105218456A (en) * | 2015-10-09 | 2016-01-06 | 株洲千金药业股份有限公司 | A kind of method of suitability for industrialized production Nitric acid butoconazole |
| CN105218455A (en) * | 2015-10-09 | 2016-01-06 | 株洲千金药业股份有限公司 | A kind of method of industrialization continuous seepage Nitric acid butoconazole |
| CN105384600A (en) * | 2015-10-09 | 2016-03-09 | 株洲千金药业股份有限公司 | Industrial production method for butoconazole nitrate intermediate |
| CN105218455B (en) * | 2015-10-09 | 2018-07-03 | 株洲千金药业股份有限公司 | A kind of method for industrializing continuous production Butoconazole Nitrate |
| CN105218456B (en) * | 2015-10-09 | 2018-07-03 | 株洲千金药业股份有限公司 | A kind of method of industrialized production Butoconazole Nitrate |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20150701 |
|
| WD01 | Invention patent application deemed withdrawn after publication |