|Company Name:||INTATRADE GmbH |
|Product Name:||BIAPENEM SIDE CHAIN|
|Synonyms:||6,7-dihydro-6-mercapto-5h-pyrazolo[1,2-a][1,2,4]triazol-4-ium chloride;6,7-DIHYDRO-6-MERCAPTO-5H-PYRAZOLO(1,2-A) (1,2,4)-TRIAZOLIUM CHLORIDE;5H-PYRAZOLO[1,2-A][1,2,4]TRIAZOL-4-IUM, 6,7-DIHYDRO-6-MERCAPTO-, CHLORIDE;Side chain for Biapenem;SIDE CHAIN FOR BIAPENEM 97+%（HPLC）;5H-Pyrazolo[1,2-a][1,2,4]triazol-4-ium,6,7-dihydr;6,7-dihydro-6-mercapto-5H-pyrazolo[1,2-a][1,2,4]triazolium chloride (the sidechain of biapenem);BIAPENEM SIDE CHAIN|
|Product Categories:||Chemical intermediate for Biapenem;API intermediates;(the sidechain of biapenem);Other Products;Pharmaceutical intermediate|
|BIAPENEM SIDE CHAIN Chemical Properties|
|BIAPENEM SIDE CHAIN Usage And Synthesis|
|Outline||Side Chain for Biapenem belongs to the raw material of medicine pharmaceutical and can be used for the production of biapenem antibiotic drugs. Biapenem (Biapenem, LJC 10627) is a kind of injection-used carbon penicillin vinyl antibiotics developed by Lederle Japan and American Cyanamid in 1989. Now the phase III clinical study has been completed in Japan and it is now waiting for approval for entering into market. The most notable feature of this product is that it is a kind of 1β- methyl carbapenem with its 2-position S containing a bi-cyclic triazole. Structure-efficacy relationship studies have showed that the presence of the side chain quaternary ammonium cation center is the key to the outer membrane permeability, making it have its inhibitory effect on Pseudomonas aeruginosa and anaerobes being 2-4 times as high as that of imipenem; its inhibitory effect on drug resistant pseudomonas aeruginosa is 4 to 8 times as high as meropenem. It is also more effective in treating Acinetobacter spp, anaerobes than ceftazidime.
|Reference quality standards||Items Standards |
Appearance: white to light yellow crystalline powder
Determination of content: 98%
Specific rotation: -26.0 ° to -36.0 °
PH: ph value should be 4.5 to 6.0
Single impurity: <1.0%
Total amount of impurities: <3.0%
Tetrahydrofuran and acetone: THF is less than 0.072%, less than 0.5% acetone
Loss on weight upon drying: not more than 1.0%
Residue upon ignition: not more than 0.2%
Heavy metals: not more than 20ppm
|The current status of Chinese imipenem drugs||Imipenem drug is by far the antibiotic with the broadest antibacterial spectrum and strong antibacterial activity and therefore plays an important role of the last-line defense for fighting against severe clinical infection. In recent years, owing to the serious issue of drug-resistant strains, there has been rapid growth of these drugs in the world and domestic usage. The world has listed six varieties including imipenem-cilastatin, panipenem-Betamipron, meropenem, biapenem (Side Chain for Biapenem), ertapenem and doripenem. However, imipenem is clinically used as second-line drugs; moreover, the guideline of government for rational application of antibiotics and its expensive price have also greatly limited the expansion of the usage number of imipenem; all these factors have determined that these drugs is still a kind of “noble” drug varieties with high additional value and small scale in the short term. |
At 2008, the terminal sales scope of imipenem in China market has reached 18.9 billion (US$ 278 million), accounting for 9% of the global total sales which is around $ 3 billion; the sales amount has reached to about 12.43 million which consumes 5-6 tons/year of raw materials from which domestic raw materials are 1.9 tons (among them, 1.8 tons are meropenem, and imipenem accounts for 0.14 tons), accounting for 36%.
In the raw materials export market, at 2008, the exports amount of the three major biapenem products in China- meropenem, imipenem and intermediate 4-AA have their raw material exports amount be 6 tons, 1.3 tons and 40 tons, respectively, which was estimated to account for over 60% of the raw material market demand of drugs with global generic name.
Since 2009, the international market demand has continuously grown. The imipenem raw material and the technology cost of the intermediate of China have gradually gained advantage, in particular has meropenem occupying a larger scale in the international market with a certain right of speech in the price. In the full year of 2009, it was expected that the export amount of meropenem and 4-AA will reach 8 tons and 50 tons, respectively with a growth rate being 30%. Imipenem drugs will continue to grow rapidly and smoothly in accordance with their own "rhythm."
The above information is edited by the Chemicalbook of Dai Xiongfeng.
|Chemical Properties||1KG; 20KG|
|BIAPENEM SIDE CHAIN Preparation Products And Raw materials|