1385033-52-2Relevant academic research and scientific papers
Synthesis of biaryl ketones by arylation of Weinreb amides with functionalized Grignard reagents under thermodynamic controlvs.kinetic control ofN,N-Boc2-amides
Li, Guangchen,Szostak, Michal
supporting information, p. 3827 - 3831 (2020/06/03)
A highly efficient method for chemoselective synthesis of biaryl ketones by arylation of Weinreb amides (N-methoxy-N-methylamides) with functionalized Grignard reagents is reported. This protocol offers rapid entry to functionalized biaryl ketones after Mg/halide exchange with i-PrMgCl·LiCl under operationally-simple and practical reaction conditions. The scope of the method is highlighted in >40 examples, including bioactive compounds and pharmaceutical derivatives. Collectively, this transition-metal-free approach offers a major advantage over the recently established cross-coupling of amides by oxidative addition of N-C(O) bonds. Considering the utility of amide acylation reactions in modern synthesis, we expect that this method will be of broad interest.
Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents
Hayashi, Yoshio,Yamazaki, Yuri,Sumikura, Makiko,Masuda, Yurika,Hayashi, Yoshiki,Yasui, Hiroyuki,Kiso, Yoshiaki,Chinen, Takumi,Usui, Takeo,Yakushiji, Fumika,Potts, Barbara,Neuteboom, Saskia,Palladino, Michael,Lloyd, George Kenneth
, p. 4279 - 4289 (2012/09/08)
KPU-105 (4), a potent anti-microtubule agent that contains a benzophenone was derived from the diketopiperazine-type vascular disrupting agent (VDA) plinabulin 3, which displays colchicine-like tubulin depolymerization activity. To develop derivatives wit
