521284-19-5Relevant articles and documents
Concise Synthesis of Key Intermediate of Mirabegron via a Mixed Anhydride Method
Zhang, Qi-Long,Zhuang, Zhi-Yuan,Liu, Qing-Dong,Zhang, Zhan-Ming,Zhan, Fu-Xu,Zheng, Geng-Xiu
, p. 1993 - 1996 (2016)
An efficiently scalable synthesis of key intermediate toward mirabegron has been developed via a mixed anhydride method, employing PivCl instead of EDCI and HOBt. The developed process produced (R)-2-hydroxy-N-(4-nitrophenethyl)-2-phenylacetamide (10) in 91.5-92.3% yield and >99.0% HPLC purity under mild conditions. During this process, a side reaction induced by triethylamine hydrochloride was discovered and investigated, which was ultimately avoided by executing the reaction in a biphasic solvent system.
A METHOD FOR PREPARING MANDELIC ACID 4-NITROPHENYL ETHYLAMIDE FROM 4-NITROBENZYL CYANIDE
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Page/Page column 11-13, (2019/05/15)
Preparation of a salt of 4-nitrophenyl ethylamine with (R)-mandelic acid and its use for the synthesis of mirabegron is disclosed. 4-Nitrophenyl ethylamine (1) is prepared by reduction of 4-nitrobenzyl cyanide (7) in a solvent with the use of a borane generated in-situ in the reaction mixture from NaBH4 and BF3.Et2O, 4-nitrophenyl ethylamine (1) being isolated from the solution as the mandelate 3.
Aryl or heteroaryl substituted pyrrolidine amide derivatives and application thereof
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Paragraph 0220-0222, (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.