1419186-19-8Relevant articles and documents
Synthesis of a spiroindolinone pyrrolidinecarboxamide MDM2 antagonist
Shu, Lianhe,Li, Zizhong,Gu, Chen,Fishlock, Dan
, p. 247 - 256 (2013)
A practical synthesis of a spiroindolinone pyrrolidinecarboxamide MDM2 antagonist 2 is reported. Cycloaddition of dipolarophile 3 with imine 30 afforded a complex mixture of diastereomers that were isomerized to the desired stereoisomer 31 by heating the mixture in the presence of DBU. After hydrolysis, the resulting product was resolved with a chiral amine to give an enantiopure acid which was converted to the target product 2. The process has been scaled up to a multihundred-gram scale. In addition, an asymmetric synthesis of 31 catalyzed by AgOAc and a chiral phosphine ligand was developed to give enantiomerically enriched 31, which was also converted to enantiopure 2.
SPIROCYCLIC INDOLONE POLYETHYLENE GLYCOL CARBONATE COMPOUND, COMPOSITION, PREPARATION METHOD AND USE THEREOF
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, (2019/06/27)
The present invention relates to a spirocyclic indolone polyethylene glycol carbonate compound, a composition thereof, a preparation method therefor, and a use thereof as an anticancer drug due to the antitumor activity thereof. The structural formula of the spirocyclic indolone polyethylene glycol carbonate compound is shown below. The compound has excellent tumor inhibitory activity, water solubility, low toxicity, and can be used for intravenous injection.
Spiroindolone polyethylene glycol carbonate compound, and compositions, preparation method and application thereof
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Paragraph 0076-0078, (2018/04/03)
The invention relates to a spiroindolone polyethylene glycol carbonate compound, compositions and a preparation method thereof, and an application of the spiroindolone polyethylene glycol carbonate compound as an anticancer drug due to antitumor activity of the spiroindolone polyethylene glycol carbonate compound. The spiroindolone polyethylene glycol carbonate compound has a structural formula asdescribed in the specification, has excellent tumor suppressive activity, good water solubility and low toxicity, and can be used for intravenous injections.