CN107540610A - A kind of production technology of side chain for biapenem product VIII - Google Patents
A kind of production technology of side chain for biapenem product VIII Download PDFInfo
- Publication number
- CN107540610A CN107540610A CN201610469512.1A CN201610469512A CN107540610A CN 107540610 A CN107540610 A CN 107540610A CN 201610469512 A CN201610469512 A CN 201610469512A CN 107540610 A CN107540610 A CN 107540610A
- Authority
- CN
- China
- Prior art keywords
- vii
- side chain
- product
- potassium hydroxide
- biapenem
- 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.)
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- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Abstract
The present invention relates to medical pharmaceutical field, more particularly, to side chain for biapenem field.You belong to medical pharmaceutical raw material by its training southern side chain, and available for production that, it trains southern antibiotic medicine.Your its training south is a kind of tribactams, by being combined with PBP, disturbs the synthesis of bacteria cell wall, causes bacterial growth reproduction inhibition system, cell dissolving occurs in minority.The product have height antibacterial activity to the gram positive bacterias such as methicillin-sensitivity S. aureus L-forms, streptococcus pneumonia, micrococcus scarlatinae, enterobacteriaceae lactobacteriaceae；Hemophilus, moraxelle catarrhalis, Neisseria meningitidis etc. are extremely sensitive to the product, but to bacteriums such as methicillin-resistant Staphylococci, enterococcus spp, pseudomonas aeruginosa, acinetobacters to the product resistance.
Description
Technical field
The present invention relates to medical pharmaceutical field, more particularly, to side chain for biapenem field.
Background technology
You belong to medical pharmaceutical raw material by its training southern side chain, and available for production that, it trains southern antibiotic medicine.You are at its training south
A kind of tribactams, by being combined with PBP, the synthesis of bacteria cell wall is disturbed, caused thin
There is cell dissolving in bacteria growing reproduction inhibition system, minority.The product are to methicillin-sensitivity S. aureus L-forms, streptococcus pneumonia, suppurative
The gram positive bacterias such as streptococcus, enterobacteriaceae lactobacteriaceae have height antibacterial activity；Hemophilus, moraxelle catarrhalis, meningitis
Neisser's coccus etc. is extremely sensitive to the product, but to methicillin-resistant Staphylococci, enterococcus spp, pseudomonas aeruginosa, motionless
The bacteriums such as Bacillus are to the product resistance.
The content of the invention
Technological process
Oxidation
Potassium hydroxide, vacuum suction methanol are manually added into VII stills for air blowing at room temperature, stirring reaction 20min, VII is containing hydrogen
Alcoholysis generation VII, potassium formate and methyl acetate in the methanol of potassium oxide, it is pumped into formic acid, artificial addition to middle vacuum after completion of the reaction
Potassium hydroxide.Again to middle addition catalyst ferric trichloride, normal pressure, O2 is slowly introducing at room temperature, VII occurs oxidation reaction generation VIII
And water（VII conversion ratio is 75%）, catalyst ferric trichloride is then filtered out using filter, filtrate is evacuated to Ⅸ synthesis reactor.Oxidation is anti-
Answer excessive oxygen.
Reaction principle：
The reaction equation of intermediate products VIII
Side reaction：
。
Claims (2)
1. the present invention relates to material composition and proportioning；
The present invention relates to technological process：Potassium hydroxide, vacuum suction methanol are manually added into VII stills for air blowing at room temperature, stirring is anti-
Answer 20min, VII in the methanol containing potassium hydroxide alcoholysis generation VII, potassium formate and methyl acetate, it is true in after completion of the reaction
Sky is pumped into formic acid, manually adds potassium hydroxide.
2. normal pressure, being slowly introducing O2 at room temperature to middle addition catalyst ferric trichloride again, VII occurs oxidation reaction generation VIII and water
（VII conversion ratio is 75%）, catalyst ferric trichloride is then filtered out using filter, filtrate is evacuated to Ⅸ synthesis reactor；Oxidation reaction mistake
Measure oxygen.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610469512.1A CN107540610A (en) | 2016-06-26 | 2016-06-26 | A kind of production technology of side chain for biapenem product VIII |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610469512.1A CN107540610A (en) | 2016-06-26 | 2016-06-26 | A kind of production technology of side chain for biapenem product VIII |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107540610A true CN107540610A (en) | 2018-01-05 |
Family
ID=60961088
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610469512.1A Pending CN107540610A (en) | 2016-06-26 | 2016-06-26 | A kind of production technology of side chain for biapenem product VIII |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107540610A (en) |
-
2016
- 2016-06-26 CN CN201610469512.1A patent/CN107540610A/en active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20180105 |