168133-85-5Relevant academic research and scientific papers
Carbolines, part VI. First total synthesis of Bauerine B and its demethyl analogue
Rocca,Marsais,Godard,Queguiner
, p. 2901 - 2908 (1995)
Short and convergent syntheses of Bauerine B and its demethyl analogue are reported. The approach is based on a convergent methodology which involves such reactions as metalation, heteroring cross-coupling and cyclization.
Preparation method of ortho-amino trifluoroacetophenone and derivatives thereof
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Paragraph 0041; 0045-0048, (2021/11/19)
The invention relates to the field of organic synthesis, in particular to a preparation method of ortho-amino trifluoroacetophenone and derivatives thereof. The preparation of ortho-amino trifluoroacetophenone comprises three steps of amino protection, trifluoroacetylation and deprotection, the overall reaction condition is mild, the yield is high, and the method is suitable for large-scale production. In addition, on the basis of the preparation, substitution is carried out after amino diazotization, the ortho-amino trifluoroacetophenone derivative is further prepared, and the industrial application prospect is good.
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists
Shimada, Itsuro,Maeno, Kyoichi,Kazuta, Ken-ichi,Kubota, Hideki,Kimizuka, Tetsuya,Kimura, Yasuharu,Hatanaka, Ken-ichi,Naitou, Yuki,Wanibuchi, Fumikazu,Sakamoto, Shuichi,Tsukamoto, Shin-ichi
, p. 1966 - 1982 (2008/09/21)
A series of novel indazole derivatives were synthesized, and their structure-activity relationships examined in order to identify potent and selective 5-HT2C receptor agonists. Among these compounds, (S)-2-(7-ethyl-1H-furo[2,3-g]indazol-1-yl)-1-methylethylamine (YM348) had a good in vitro profile, that is, high agonistic activity to the human 5-HT2C receptor subtype (EC50 = 1.0 nM) and high selectivity over 5-HT2A receptors. This compound was also effective in a rat penile erection model when administered po.
