77069-15-9Relevant academic research and scientific papers
NOVEL COMPOUND, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Paragraph 0453-0456, (2017/09/26)
The present invention relates to a novel compound controlling the phosphorylation of PPARandgamma; by CDK5, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The novel compound of the present invention combines t
Fused [d]pyridazin-7-ones
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Page/Page column 22, (2008/06/13)
The present invention is directed to fused [d]pyridazin-7-ones. The invention is also directed to methods for making and using the fused [d]pyridazin-7-ones. In particular, the compounds of the present invention may be effective in the treatment of diseases or disease states related to the activity of VEGFR2, MLK1 and CDK5 enzymes, including, for example, angiogenic disorders and neurodegenerative diseases.
Synthetic Studies on Indoles and Related Compounds. XV. An Unusual Acylation of Ethyl Indole-2-Carboxylate in the Friedel-Crafts Acylation
Murakami, Yasuoki,Tani, Masanobu,Tanaka, Kenjiro,Yokoyama, Yuusaku
, p. 2023 - 2035 (2007/10/02)
The Friedel-Crafts reaction of ethyl indole-2-carboxylate (1a) with acyl chlorides or acid anhydrides in the presence of Lewis acids was investigated in order to establish a preparative procedure for the corresponding ethyl 3-acylindole-2-carboxylates (4).Although monoacylation occured successfully, the products were generally a mixture of ethyl 3-, 5-, and 7-acylindole-2-carboxylates (4,5 and 6).The ratio of the yields of these three products varied greatly depending on reaction conditions and reagents used.A tendency that the 3-acylindole (4) was obtained as a main product was observed when a Lewis acid other than aluminum chloride was used as a catalyst and/or an acyl chloride derived from a weaker acid was employed, whereas a tendency for formation of the 5- and 7-acylindoles (5 and 6) was observed when aluminum chloride and/or an acyl chloride derived from a stronger acid was used.As to the 5- and 7-acylindoles (5 and 6) , the yields of the former were always much higher than those of the latter (6).The result indicates that ethyl 3- and 5-acylindole-2-carboxylates can be regioselectively prepared from a common substrate (1a) by changing the reaction conditions or reagents. friedel-craft acylation; ethyl indole-2-carboxylate; acyl chloride; acid anhydride; lewis acid; aluminum chloride; acylindole
THE FRIEDEL-CRAFTS ACYLATION OF ETHYL INDOLE-2-CARBOXYLATE. AN USUAL SUBSTITUTION ON THE BENZENE MOIETY.
Murakami, Yasuoki,Tani, Masanobu,Tanaka, Kenjiro,Yokoyama, Yuusaku
, p. 241 - 244 (2007/10/02)
Ethyl indole-2-carboxylate can be acylated with a variety of acyl chlorides under Friedel-Crafts conditions to give mono-acyl indole derivatives.However, the acyl chloride derived from a stronger acid tends to substitute at the C-5 position rather than at
