361-92-2Relevant articles and documents
Identification of 2-(2′-fluoro-[1,1′-biphenyl]-2-yl)acetamide as a Sodium Valproate-like broad spectrum anti-epileptic drug candidate
Tanaka, Tomoyuki,Yajima, Nana,Kiyoshi, Tomoko,Miura, Yoshiki,Inoue, Yoshifumi,Nishimaki, Takuya,Iwama, Seiji
, p. 138 - 142 (2018/12/13)
By further optimizing compound A [2′-fluoro-N-methyl-[1,1′-biphenyl]-2-sulfonamide], we identified DSP-0565 [2-(2′-fluoro-[1,1′-biphenyl]-2-yl)acetamide, 17a] as a strong, broad-spectrum anti-epileptic drug (AED) candidate. Our efforts mainly focused on finding an alternative polar group for the sulfonamide in order to improve ADME profile of compound A including good metabolic stability and no reactive metabolic production. This led to the identification of biphenyl acetamide as a new scaffold for development of broad-spectrum AED candidates. DSP-0565 showed anti-convulsant activity in various models (scPTZ, MES, 6 Hz and amygdala kindling) with good safety margin, and was therefore selected as a clinical candidate.
Pd-catalyzed C-H lactonization for expedient synthesis of biaryl lactones and total synthesis of cannabinol
Li, Yan,Ding, Yan-Jun,Wang, Jian-Yong,Su, Yi-Ming,Wang, Xi-Sheng
supporting information, p. 2574 - 2577 (2013/07/11)
A practical Pd(II)/Pd(IV)-catalyzed carboxyl-directed C-H activation/C-O cyclization to construct biaryl lactones has been developed. The synthetic utility of this new reaction was demonstrated in an atom-economical and operationally convenient total synthesis of the natural product cannabinol from commercially available starting materials, with the newly developed method used for two key steps.
Halogen-containing, optically active liquid crystal compound and liquid crystal composition containing same
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, (2008/06/13)
A novel optically active liquid crystal compound and a liquid crystal composition containing the same are provided, which compound is expressed by the formula STR1 wherein R1 is alkyl or alkoxy of 4-18 C; R2 is alkyl, alkoxy, acyl or alkoxymethyl of 4-18 C; but either one of R1 or R2 is an optically active group; either one of X1 or X2 is halogen atom and the other is H; m and n each are 0 or 1 and m+n is 0 or 1.