10342-66-2Relevant articles and documents
Preparation method of pazopanib intermediate
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Paragraph 0157-0159, (2021/03/24)
The invention provides a preparation method of a pazopanib key intermediate 2,3-dimethyl-N-(2-chloropyrimidin-4-yl)-N-methyl-2H-indazole-6-amine. The method comprises the following steps: by taking 6-halogenated-2,3-dimethyl-2H-indazole as a raw material, conducting reacting to obtain N,2,3-trimethyl-2H-indazole-6-amine; and further carrying out a reaction to obtain the 2,3-dimethyl-N-(2-chloropyrimidin-4-yl)-N-methyl-2H-indazole-6-amine. The method has the advantages of short synthesis route, accessible raw materials, low cost, mild reaction conditions, high safety and high yield, and is suitable for industrial mass production.
AURORA AND FLT3 KINASES MODULATORS
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Page/Page column 46, (2013/08/28)
The invention provides a compound having the formula (1) useful as modulator of the activity of Aurora kinases and FLT3 kinases: and salts thereof; wherein: R1 is hydrogen or C1-2 alkyl; and R2, R3 and R4 are the same or different and each is selected from hydrogen, C1-2 alkyl, fluorine, chlorine, C1-2 alkoxy and trifluoromethyl, provided that no more than two of R2, R3 and R4 are other than hydrogen. Also provided are pharmaceutical compositions containing the compounds and their use in medicine, and in particular in the treatment of cancer
Asymmetric hydrovinylation of vinylindoles. A facile route to cyclopenta[g]indole natural products (+)-cis-trikentrin A and (+)-cis-trikentrin B
Liu, Wang,Lim, Hwan Jung,Rajanbabu
supporting information; experimental part, p. 5496 - 5499 (2012/05/20)
Vinylindoles undergo Ni(II)-catalyzed asymmetric hydrovinylation under very mild conditions (-78 °C, 1 atm ethylene, 4 mol % catalyst) to give the corresponding 2-but-3-enyl derivatives in excellent yields and enantioselectivities. Hydroboration of the alkene and oxidation to an acid, followed by Friedel-Crafts annulation, gives an indole-annulated cyclopentanone that is a suitable precursor for the syntheses of cis-trikentrins and all known herbindoles. For example, the cyclopentanone from 4-ethyl-7-vinylindole is converted into (+)-cis-trikentin A in four steps (Wittig reaction, alkene isomerization, diastereoselective hydrogenation, and nitrogen deprotection). The previous synthesis of this molecule from (S)-(-)-malic acid involved more than 20 steps and a preparative HPLC separation of diastereomeric intermediates.