- Synthesis of novel indole-benzimidazole derivatives
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2-Methylindole-3-acetic acid and its 5-methoxy derivative were prepared from the respective phenylhydrazines and levulinic acid. Indole-3-carboxylic acid was obtained from indole, dimethylformamide and trifluoroacetic acid. These indole carboxylic acids were then condensed with substituted o-phenylenediamines under high temperature conditions in the presence of polyphosphoric acid as a catalyst to give the combined indole-benzimidazoles.
- Wang, Xinying,Liu, Yizhou,Xu, Juan,Jiang, Fanwei,Kang, Congmin
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- Rapid access to spirocyclized indolenines via palladium-catalyzed cascade reactions of tryptamine derivatives and propargyl carbonate
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We report the intermolecular palladium-catalyzed reaction of tert-butyl propargyl carbonate with tryptamine derivatives or other indole-containing bis-nucleophiles. The reaction proceeds under mild conditions and with low catalyst loadings to afford novel spiroindolenine products in good to high yields.
- Montgomery, Thomas D.,Nibbs, Antoinette E.,Zhu, Ye,Rawal, Viresh H.
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p. 3480 - 3483
(2014/07/21)
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- Discovery of selective indole-based prostaglandin D2 receptor antagonist
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A series of N-benzoyl-2-methylindole-3-acetic acids were synthesized and biologically evaluated as prostaglandin (PG) D2 receptor antagonists. Some of the selected compounds significantly inhibited OVA-induced vascular permeability in guinea pig conjunctiva after oral dosing. Structure-activity relationship study is presented.
- Iwahashi, Maki,Shimabukuro, Atsushi,Onoda, Takahiro,Matsunaga, Yoko,Okada, Yutaka,Matsumoto, Ryoji,Nambu, Fumio,Nakai, Hisao,Toda, Masaaki
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p. 4574 - 4588
(2011/09/19)
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- Hypoglycemic imidazoline compounds
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This invention relates to certain novel imidazoline compounds and analogues thereof, to their use for the treatment of diabetes, diabetic complications, metabolic disorders, or related diseases where impaired glucose disposal is present, to pharmaceutical compositions comprising them, and to processes for their preparation.
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- A convenient method for the synthesis of indole-3-acetic acids
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Starting from the corresponding indoles, indole-3-acetic acids were synthesized through indole-3-glyoxylic acids, followed by hydrazone formation with p-toluenesulfonhydrazide, then reduction of the hydrazones with sodium borohydride.
- Guan, Xiangming,Borchardt, Ronald T.
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p. 3013 - 3016
(2007/10/02)
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