147124-34-3Relevant academic research and scientific papers
Probing cytochrome P450 (CYP) bioactivation with chloromethylindoline bioprecursors derived from the duocarmycin family of compounds
Ortuzar, Natalia,Karu, Kersti,Presa, Daniela,Morais, Goreti R.,Sheldrake, Helen M.,Shnyder, Steve D.,Barnieh, Francis M.,Loadman, Paul M.,Patterson, Laurence H.,Pors, Klaus,Searcey, Mark
, (2021/05/04)
The duocarmycins belong to a class of agent which has great potential for use in cancer therapy. Their exquisite potency means they are too toxic for systemic use, and targeted approaches are required to unlock their clinical potential. In this study, we
Preparation method for 5-fluoroindole-2-ketone
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Paragraph 0009; 0021; 0035; 0036; 0040; 0041; 0045; 0046, (2018/12/13)
The invention discloses a preparation method for 5-fluoroindole-2-ketone. The preparation method comprises the following steps: taking 2,4-difluoronitrobenzene as a raw material, enabling the 2,4-difluoronitrobenzene to perform condensation reaction with dimethyl malonate in an aprotic polar solvent under an inorganic alkaline condition, and performing post-treatment to obtain 4-fluoro-2-(dimehtylmalonate) nitrobenzene; in the presence of the aprotic polar solvent and lithium chloride, enabling the 4-fluoro-2-(dimehtyl malonate) nitrobenzene to generate 5-fluoro-2- nitrobenzene methyl acetate; mixing the 5-fluoro-2- nitrobenzene methyl acetate, a catalyst and alcohol solvents to perform hydrogenation cyclization reaction to obtain a 5-fluoroindole-ketone crude product; taking water as thesolvent by the crude product, filtering active carbon while hot, and re-crystallizing to obtain high-purity 5-fluoro-indole-2-ketone. The method adopts easily available raw materials, is simple in process; and a Raney nickel catalyst and a recrystallization aqueous solution can be used for many times, the raw material cost is relatively low, industrialization is easily realized, and the application prospect is relatively great.
Asymmetic organocatalytic 1,3-dipolar cycloaddition of azomethine ylide to methyl 2-(2-nitrophenyl)acrylate for the synthesis of diastereoisomers of spirotryprostatin A
Cheng, Mou-Nuo,Wang, Hao,Gong, Liu-Zhu
supporting information; experimental part, p. 2418 - 2421 (2011/06/23)
Chemical equations presented. The total synthesis of two diastereomers of spirotryprostatin A has been established starting with an asymmetric 1,3-dipolar cycloaddition of methyl 2-(2-nitrophenyl)acrylate with azomethine ylides catalyzed by a Bronsted aci
COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
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Page/Page column 43-44, (2010/11/30)
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly di
2-CYANOPYRROLOPYRIMIDINES AND PHARMACEUTICAL USES THEREOF
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Page/Page column 43-44, (2010/02/08)
The invention relates to pyrrolo pyrimidines of formula (I), wherein Y represents -(CH2)t-O- or -(CH2)r-S-, p is 1 or 2, r is 1, 2 or 3, t is 1, 2 or 3, or Y is -(CH2)j- or -CH=CH-, j is 1 or 2; p is 1 or 2, or Y is -(CH2)f-, f is 1 or 2, p is 1, and the further radicals and symbols have the meaning as defined herein; their preparation, their use as pharmaceuticals, pharmaceutical compositions containing them, the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment of neuropathic pain and to a method for the treatment of such a disease in animals, especially in humans.
Process for producing 5-fluorooxyindole and for producing intermediates therefor
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, (2008/06/13)
The present invention discloses a process for preparing 5-fluorooxindole represented by the formula (3): which comprises (A) a first step of cyclizing 2-(5-fluoro-2-nitrophenyl)malonic acid diester represented by the formula (1) : wherein R1 an
A direct synthesis of 2-arylpropenoic acid esters having nitro groups in the aromatic ring: A short synthesis of (±)-coerulescine and (±)-horsfiline
Selvakumar,Azhagan, A.Malar,Srinivas,Krishna, G.Gopi
, p. 9175 - 9178 (2007/10/03)
A short synthesis of 2-arylpropenoic acid esters that possess nitro groups in their phenyl ring using common and less expensive reagents is described. The usefulness of this methodology is substantiated by the efficient total syntheses of (±)-coerulescine and (±)-horsfiline from the 2-arylpropenoic acid esters obtained.
A general oxindole synthesis
Quallich,Morrissey
, p. 51 - 53 (2007/10/02)
A general synthesis of indol-2(3H)-ones (oxindoles), was developed based on the addition of dimethyl malonate to commercially available halonitrobenzenes. The advantage of this route over many other oxindole syntheses was the regiochemical control of the substitution pattern on the aromatic ring.
