41780-52-3Relevant articles and documents
INHIBITORS OF THE N-TERMINAL DOMAIN OF THE ANDROGEN RECEPTOR
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Page/Page column 57; 63, (2020/10/20)
The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.
Process method suitable for amplification preparation of 4-(6-aminopyridin-3-yl) substituted piperidine
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Paragraph 0069-0071; 0072, (2019/12/25)
The invention discloses a process method suitable for amplification preparation of 4-(6-aminopyridin-3-yl) substituted piperidine, and belongs to the synthesis field of a medicine intermediate. N-substituted piperidone, aryl sulfohydrazide and 2-amino-5-bromopyridine are subjected to a coupling reaction under a palladium catalyst, and then are subjected to a hydrogenation to obtain 4-(6-aminopyridin-3-yl) substituted piperidine. According to the process, the raw materials in pyridine do not need to be protected; the condensation and the coupling are carried out in the same reaction kettle, sothat the operation cost is reduced, the steps of performing protection at first and then performing protection removal as in documents can be avoided, and production cost of the existing biological, medicine and chemical intermediates is greatly reduced; and the process is subjected to amplification verification in kilogram-scale, and the verification proves that the yield and the product purity are basically equal to those of gram-scale, so that the method can be used as a process for industrial scale production.
Difunctionalization of ketones: Via gem -bis(boronates) to synthesize quaternary carbon with high selectivity
Zheng, Purui,Zhai, Yujie,Zhao, Xiaoming,Xu, Tao
supporting information, p. 13375 - 13378 (2018/12/13)
All-carbon quaternary centres are significant and prevalent structural frameworks but their preparation routes are rare and challenging, especially methods with common substrates. Herein, we report a convenient process to construct all-carbon quaternary c