7023-79-2Relevant academic research and scientific papers
Synthesis of the Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor NB-360
Rueeger, Heinrich,Lueoend, Rainer,Machauer, Rainer,Veenstra, Siem J.,Holzer, Philipp,Hurth, Konstanze,Voegtle, Markus,Frederiksen, Mathias,Rondeau, Jean-Michel,Tintelnot-Blomley, Marina,Jacobson, Laura H.,Staufenbiel, Matthias,Laue, Grit,Neumann, Ulf
supporting information, p. 4677 - 4696 (2021/05/06)
Starting from lead compound 4, the 1,4-oxazine headgroup was optimized to improve potency and brain penetration. Focusing at the 6-position of the 5-amino-1,4-oxazine, the insertion of a Me and a CF3 group delivered an excellent pharmacological profile wi
Tandem Synthesis of α-Diazoketones from 1,3-Diketones
Zhang, Jianlan,Chen, Wenwen,Huang, Dayun,Zeng, Xiaobao,Wang, Xinyan,Hu, Yuefei
, p. 9171 - 9174 (2017/09/11)
A highly efficient synthesis of α-diazoketone was achieved by simply stirring the mixture of 1,3-diketone, TsN3, and MeNH2 in EtOH. It was a tandem reaction including a novel primary amine-catalyzed Regitz diazo transfer of 1,3-diket
One-pot synthesis of polyfunctional pyrazoles: An easy access to α-diazoketones from arylglyoxal monohydrates and tosylhydrazine
Shu, Wen-Ming,Ma, Jun-Rui,Zheng, Kai-Lu,Sun, Hui-Ying,Wang, Mei,Yang, Yan,Wu, An-Xin
, p. 9321 - 9329 (2015/03/05)
A new and efficient method for the generation of α-diazoketones has been developed from arylglyoxal monohydrates and tosylhydrazine at room temperature. 1,3-Dipolar cycloaddition reactions were used to constructing polyfunctional pyrazole derivatives by the reaction of generated α-diazoketones in situ with electron-deficient alkenes, quinones and coumarins in one pot. The one-dimensional molecular packing of 1H-benzo[f]indazole-4,9-dione derivatives along the c direction demonstrated a helical chain formation via N-H?O hydrogen-bonding.
Quinolones as gonadotropin releasing hormone (GnRH) antagonists: Simultaneous optimization of the C(3)-aryl and C(6)-substituents
Young, Jonathan R.,Huang, Song X.,Chen, Irene,Walsh, Thomas F.,DeVita, Robert J.,Wyvratt Jr., Matthew J.,Goulet, Mark T.,Ren, Ning,Lo, Jane,Yang, Yi Tien,Yudkovitz, Joel B.,Cheng, Kang,Smith, Roy G.
, p. 1723 - 1727 (2007/10/03)
A series of 3-arylquinolones was prepared and evaluated for their ability to act as gonadotropin releasing hormone (GnRH) antagonists. A variety of substitution patterns of the 3-aryl substituent are described. The 3,4,5-trimethylphenyl substituent (23h) was found to be optimal. (C) 2000 Elsevier Science Ltd. All rights reserved.
