- An optimized procedure for direct access to 1: H -indazole-3-carboxaldehyde derivatives by nitrosation of indoles
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Indazole derivatives are currently drawing more and more attention in medicinal chemistry as kinase inhibitors. 1H-indazole-3-carboxaldehydes are key intermediates to access to a variety of polyfunctionalized 3-substituted indazoles. We report here a general access to this motif, based on the nitrosation of indoles in a slightly acidic environment. These very mild conditions allow the conversion of both electron-rich and electron-deficient indoles into 1H-indazole-3-carboxaldehydes.
- Chevalier, Arnaud,Ouahrouch, Abdelaaziz,Arnaud, Alexandre,Gallavardin, Thibault,Franck, Xavier
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p. 13121 - 13128
(2018/04/23)
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- ANTICANCER AGENT
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An anticancer agent comprising a compound represented by the formula (I) [R1 represents hydrogen atom, hydroxyl group, a C1-6alkoxy group and the like; R2 and R3 represents hydrogen atom, a halogen atom, a C1-6alkyl group and the like; R4 represents hydrogen atom, a C1-6alkyl group, a C1-6alkylsulfonyl group and the like; R5 represents hydrogen atom or a substituent; .... represents a single bond or a double bond; R6 and R7 represents hydrogen atom, a C1-6alkyl group and the like; R8 represents hydrogen atom, a C1-6alkyl group and the like; A represents -O-, -S-, or - CH2-; D represents -C= or -N=; X represents methylene group, -O-, or -CO-; Q represents -N= or -C(R8)=; and Y represents a heterocyclic group or amino group], which shows a superior inhibitory activity against pim-1 kinase.
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Paragraph 0359
(2013/03/26)
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- Indazole benzimidazole compounds
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Organic compounds having the structure I are provided where the variables have the values described herein. Pharmaceutical formulations and medicaments include the organic compound or a pharmaceutically acceptable salt thereof and a pharmaceutically accep
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Page/Page column 85
(2008/06/13)
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- Direct Acting, Highly Mutagenic, α-Hydroxy N-Nitrosamines from 4-Chloroindoles
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Fave beans (Vicia fava) contain 4-chloro-6-methoxyindole, a promutagen, which on nitrosation under simulated gastric conditions forms 4-chloro-6-methoxy-2-hydroxy-N1-nitrosoindolin-3-one oxime, a direct-acting, exceedingdly potent, mutagen whic
- Buechi, George,Lee, Gary C. M.,Yang, David,Tannenbaum, Steven R.
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p. 4115 - 4119
(2007/10/02)
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