223673-34-5Relevant articles and documents
Targeting a Mirabegron precursor by BH3-mediated continuous flow reduction process
De Angelis, Sonia,Carlucci, Claudia,de Candia, Modesto,Rebuzzini, Gabriele,Celestini, Paolo,Riscazzi, Massimiliano,Luisi, Renzo,Degennaro, Leonardo
, p. 81 - 85 (2018)
A continuous-flow reduction of (R)-2-hydroxy-N-[2-(4-nitrophenyl)ethyl]-2-phenylacetamide, involved in the synthetic pathway of Mirabegron, has been developed. This study demonstrated the possibility to safely handling BH3 complexes within microfluidic reactors using 2-MeTHF as greener alternative to traditional solvents, and without requiring any additive such as DMI. In addition, NMR and HPLC purity analysis revealed that the sole by-product of this process is the diamine 3, which wouldn't affect the following synthetic steps towards Mirabegron.
Aryl or heteroaryl substituted pyrrolidine amide derivatives and application thereof
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Paragraph 0223-0226, (2019/05/22)
The invention discloses aryl or heteroaryl substituted pyrrolidine amide derivatives and an application thereof, in particular to a novel aryl or heteroaryl substituted pyrrolidine amide derivative and a pharmaceutical composition containing the same, which can be used for activating beta3-adrenergic receptor. The invention also relates to a method for preparing the compounds and pharmaceutical compositions, as well as an application thereof in preparing drugs for treating diseases or symptoms mediated by beta3-adrenergic receptor, and especially for treating the overactive bladder.
Acyl-substituted pyrrolidine amide derivative and application thereof
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Paragraph 0234; 0239; 0240; 0241, (2019/06/12)
The invention discloses an acyl-substituted pyrrolidine amide derivative and application thereof. Specifically, the invention relates to a novel acyl-substituted pyrrolidine amide derivative and a pharmaceutical composition containing the compound, which can be used for activation of beta3-adrenoceptor. The invention also relates to a method for preparing the compound and the pharmaceutical composition and their application in the preparation of beta3-adrenoceptor activation-mediated diseases or symptoms, especially overactive bladder.