Method for the Production of Thiocarbamate Derivatives A2AR Inhibitors
AssigneeiTeos Belgium SA
InventorsXuecheng Jiao, Michael Deligny, Stefano Crosignani, Xiangjun Jiang
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Abstract
The present disclosure relates to synthesis of enantiomerically rich key drug intermediates as a means for manufacturing of thiocarbamate derivatives as A2A adenosine receptor (A2AR) inhibitors. More particularly, the present disclosure provides a viable efficient technology using enzymatic biotransformation process which utilizes cheaper substrate for production of high value key intermediates for A2AR inhibitors.
Claims24
A process for preparing (+)-1-(2,4-difluoro-5-(2-(methylsulfinyl)ethoxy)phenyl)piperazine (Intermediate B), or a pharmaceutically acceptable salt or solvate thereof,
- comprising the step of contacting 1-(2,4-difluoro-5-(2-(methylthio)ethoxy)phenyl)piperazine, or a pharmaceutically acceptable salt thereof:
- with an enzyme in a solvent.
A compound of formula Intermediate B:
- or a pharmaceutically acceptable salt thereof obtained by the step of contacting 1-(2,4-difluoro-5-(2-(methylthio)ethoxy)phenyl)piperazine, or a pharmaceutically acceptable salt thereof:
- with an enzyme in a solvent.
Dependencies are inferred from the claim text.