81030-75-3

Upstream product

• 22818-40-2 D-4-hydroxyphenylglycine 
• 551-16-6 6-Aminopenicillanic Acid 
• 43189-12-4 (R)-methyl 2-amino-2-(4-hydroxyphenyl)acetate 
• 54397-23-8 D-(-)-4-hydroxyphenylglycineamide 
• 732216-08-9 famotidine 
• 51481-61-9 cimetidine 
• 69-65-8 mannitol 
• 73590-58-6 omeprazole 
• 79-22-1 methyl chloroformate 
• 551-16-6 6-aminopenicillanic acid 
• 822-39-9 2-chloro-1,3,2-dioxaphospholan 
• 82095-48-5 D(-)-p-hydroxy-N-(1-ethoxycarbonyl-2-propenyl)-alpha-aminophenylacetic acid potassium salt 
• 68698-88-4 N-triisopropylsilyl-2-oxazolidinone 
• 10416-58-7 N,N-bis(trimethylsilyl)acetamide 

Downstream Products

• 129880-95-1 6-[2-(4-Hydroxy-phenyl)-2-(5-isobutyl-6-thioxo-[1,3,5]thiadiazinan-3-yl)-acetylamino]-3,3-dimethyl-7-oxo-4-thia-1-aza-bicyclo[3.2.0]heptane-2-carboxylic acid 
• 129867-34-1 6-[2-(5-Butyl-6-thioxo-[1,3,5]thiadiazinan-3-yl)-2-(4-hydroxy-phenyl)-acetylamino]-3,3-dimethyl-7-oxo-4-thia-1-aza-bicyclo[3.2.0]heptane-2-carboxylic acid 
• 129867-37-4 6-{2-(4-Hydroxy-phenyl)-2-[5-(3-methyl-butyl)-6-thioxo-[1,3,5]thiadiazinan-3-yl]-acetylamino}-3,3-dimethyl-7-oxo-4-thia-1-aza-bicyclo[3.2.0]heptane-2-carboxylic acid 
• 129867-35-2 6-[2-(4-Hydroxy-phenyl)-2-(5-pentyl-6-thioxo-[1,3,5]thiadiazinan-3-yl)-acetylamino]-3,3-dimethyl-7-oxo-4-thia-1-aza-bicyclo[3.2.0]heptane-2-carboxylic acid 
• 129867-38-5 6-[2-(5-Benzyl-6-thioxo-[1,3,5]thiadiazinan-3-yl)-2-(4-hydroxy-phenyl)-acetylamino]-3,3-dimethyl-7-oxo-4-thia-1-aza-bicyclo[3.2.0]heptane-2-carboxylic acid 
• 129867-40-9 6-[2-(5-Furan-2-ylmethyl-6-thioxo-[1,3,5]thiadiazinan-3-yl)-2-(4-hydroxy-phenyl)-acetylamino]-3,3-dimethyl-7-oxo-4-thia-1-aza-bicyclo[3.2.0]heptane-2-carboxylic acid 
• 129867-39-6 6-[2-(4-Hydroxy-phenyl)-2-(5-phenethyl-6-thioxo-[1,3,5]thiadiazinan-3-yl)-acetylamino]-3,3-dimethyl-7-oxo-4-thia-1-aza-bicyclo[3.2.0]heptane-2-carboxylic acid 

Relevant academic research and scientific papers

Amoxicillin Inactivation by Thiol-Catalyzed Cyclization Reduces Protein Haptenation and Antibacterial Potency

Serum and cellular proteins are targets for the formation of adducts with the β-lactam antibiotic amoxicillin. This process could be important for the development of adverse, and in particular, allergic reactions to this antibiotic. In studies exploring protein haptenation by amoxicillin, we observed that reducing agents influenced the extent of amoxicillin-protein adducts formation. Consequently, we show that several thiol-containing compounds, including dithiothreitol, N-acetyl-L-cysteine, and glutathione, perform a nucleophilic attack on the amoxicillin molecule that is followed by an internal rearrangement leading to amoxicillin diketopiperazine, a known amoxicillin metabolite with residual activity. Increased diketopiperazine conversion is also observed with human serum albumin but not with L-cysteine, which mainly forms the amoxicilloyl amide. The effect of thiols is catalytic and can render complete amoxicillin conversion. Interestingly, this process is dependent on the presence of an amino group in the antibiotic lateral chain, as in amoxicillin and ampicillin. Furthermore, it does not occur for other β-lactam antibiotics, including cefaclor or benzylpenicillin. Biological consequences of thiol-mediated amoxicillin transformation are exemplified by a reduced bacteriostatic action and a lower capacity of thiol-treated amoxicillin to form protein adducts. Finally, modulation of the intracellular redox status through inhibition of glutathione synthesis influenced the extent of amoxicillin adduct formation with cellular proteins. These results open novel perspectives for the understanding of amoxicillin metabolism and actions, including the formation of adducts involved in allergic reactions.

Preparation method of amoxicillin

The invention provides a preparation method of amoxicillin. The amoxicillin is obtained by synthesis of amino protected raw materials, the reaction route is short, product purity is high, operation iseasy, and wide industrial application prospects are achieved.

Purification of amoxicillin trihydrate by impurity-coformer complexation in solution

In this work, we demonstrated the purification of amoxicillin trihydrate (AMCT) by the formation of 4-hydroxyphenylglycine (4HPG)-coformer complex in solution. Without advanced knowledge of cocrystal formation of 4HPG, a workflow was established to choose

Pharmaceutical Composition for the Eradication of Helicobacter Pylori and Preparation Method Thereof

The present invention relates to a pharmaceutical composition and its preparation method for the eradication of Helicobacter pylorif in the forms of effervescent tablet, suspension or powder. The pharmaceutical composition comprises an effective dose of β-lactam antibiotic, an effective dose of macrolide antibiotic, an effective dose of antacid such as proton pump inhibitor and H2 blocker, and a pharmaceutical acceptable carrier. An effective dose of alkaline substance such as carbonate or bicarbonate can be added to increase the pH of the stomach when the PPI antacid is used, which can protect the degradation of acid-labile antibiotics or PPI to further increase the bioavailability of the pharmaceutical composition for the purpose of Helicobacter pylori eradication.

Process and device for producing liquid dosage formulations of medicinal compounds on demand from tablets and capsules

The present invention provides a process for preparing liquid pharmaceutical formulations on demand from tablets and capsules.

Method of using deuterated calcium channel blockers

Therapeutic methods and compositions using deuterated enriched 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylic acid 3-ethyl 5-methyl ester and other deuterated dihydropyridine compounds are described. The deuterated compounds exhibit enhanced efficacy in blocking calcium channels over non-deuterated dihydropyridines.

Pharmaceutical formulations containing clavulanic acid and an antibacterial agent

A method of use of clavulanate to enhance the antibacterial activity of an antibacterial compound against microorganisms having an antibiotic resistance mechanism other than β-lactamase enzyme mediated resistance. Pharmaceutical formulations and methods of use which exploit this method.

Preparation of beta-lactam antibiotics in the presence of urea or amide

A process for the preparation of β-lactam compounds has been described wherein before the addition of a base, urea or derivatives thereof and/or amide or derivatives has been added to (a) before an acid hydrolysis of the Dane salt coupling reaction mixture resulting from acylation of 6-amino-penicillanic acid, 7-amino-cephalosporanic acid or 7-amino-3'-desacetoxycephalosporanic acid and derivatives thereof at low temperature or to (b) a solution obtained by the addition of an acid to the crude β-lactam antibiotic compound in water and/or one or more organic solvents.

Penicillin acylase in the industrial production of β-lactam antibiotics

Immobilized penicillin acylase is a biocatalyst suitable for the kinetically controlled industrial synthesis of semi-synthetic antibiotics in aqueous environments. Amoxiciliin and ampicillin are obtained by condensing 6-aminopenicillanic acid with the amide or ester of D-( - )-4-hydroxyphenyIglycine and D-( - )phenylglycine, respectively. Similarly, the cephalosporin antibiotics cefadroxil and cephalexin can be obtained from 7-aminodesacetoxycephalosporanic acid.

Enhancement of the efficacy of nifedipine by deuteration

A method of enhancing the efficiency and increasing the duration of action of drugs (e.g. dihydropyridines and anti-bacterials) and particularly of nifedipine and penicillins wherein one or more hydrogen atoms are deuterated and wherein the deuterated drug has unexpectedly improved properties when used in much lower concentrations than unmodified drug. A method for determining the identity and bioequivalency of a new drug is also disclosed wherein the molecular and isotope structure of a new drug is determined by isotope ratio mass spectrometry and compared with the molecular and isotope structure of a known human drug.