396730-17-9Relevant academic research and scientific papers
Synthesis method of trelagliptin intermediate
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, (2021/07/17)
The invention belongs to the technical field of medicines, and particularly relates to a synthesis method of a trelagliptin intermediate (R)-3-aminopiperidine dihydrochloride. The synthesis method specifically comprises the following steps: 1) reducing carbonyl of a compound shown as a formula I in an organic solvent A by using a reducing agent to prepare a compound shown as a formula II; 2) splitting the compound shown in the formula II in an organic solvent B through a chiral reagent to prepare a compound shown in a formula III; and 3) removing the benzyl of the compound shown by the formula III by palladium on carbon to obtain the (R)-3-aminopiperidine dihydrochloride. The (R)-3-aminopiperidine dihydrochloride prepared by the method has high yield and purity, the HPLC purity is higher than 98.16%, and the optical purity is higher than 98.92%; and the synthesis method has the advantages of low price of initial raw materials, facilitation of reduction of industrial cost, short synthesis process route, mild reaction conditions and easy industrial realization.
Heterocyclic compounds as inhibitors of beta-lactamases
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, (2008/06/13)
This invention discloses and claims methods for inhibiting bacterial β-lactamases and treating bacterial infections by inhibiting bacterial β-lactamases in man or an animal comprising administering a therapeutically effective amount to said man or said animal of a compound, or pharmaceutically acceptable salt thereof, of formula (I) either alone or in combination with a β-lactamine antibiotic wherein said combination can be administered separately, together or spaced out over time. Pharmaceutical compositions comprising a compound of formula (I), or a combination of a compound of formula (I) and a therapeutically effective amount of a β-lactamine antibiotic, and a pharmaceutically acceptable carrier are also disclosed and claimed. 1
Azabicyclic compounds, preparation thereof and use as medicines, in particular as antibacterial agents
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Page/Page column 17, (2010/11/30)
The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds as well as their use as medicaments, in particular as anti-bacterial agents.
