717843-48-6Relevant articles and documents
IMIDAZOPYRIMIDINES AS EED INHIBITORS AND THE USE THEREOF
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, (2021/02/12)
The present disclosure provides compounds represented by Formula (I) wherein R1, R2, R3, and R4 are as defined in the specification, and the salts and solvates thereof. Compounds of Formula (I) are FED inhibitors. FED inhibitors are useful for the treatment of cancer and other diseases.
FUSED HETEROCYCLIC DERIVATIVES, THEIR PREPARATION METHODS THEREOF AND MEDICAL USES THEREOF
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, (2019/07/03)
The present invention relates to fused heterocyclic derivatives, processes for their preparation and their use in medicine. Specifically, the present invention relates to a novel derivative represented by the formula (I′), or its pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the derivative or its pharmaceutically acceptable salt thereof, and the method for preparing the derivative and its pharmaceutically acceptable salt thereof. The present invention also relates to the use of the derivative and its pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing the derivative and its pharmaceutically acceptable salt thereof in the preparation of medicines, in particularly as IDO inhibitor medicines, for treating and/or preventing cancers. Wherein each substituent of the formula (I′) is the same as defined in the specification.
Method for totally synthesizing natural product (+/-)-rupestine G and resolving enantiomers
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, (2017/09/13)
The invention relates to a method for totally synthesizing a natural product (+/-)-rupestine G and resolving enantiomers. The method comprises the following steps: oxidizing the raw material 2-methyl-5-bromopyridine (1) by m-chloroperoxybenzoic acid to obtain a nitrogen oxidation product compound 2, carrying out a Reissert-Henze reaction to perform cyano substitution so as to obtain a compound 3, carrying out a decarboxylation reaction on the compound 3 and potassium monoethyl malonate to obtain beta-ketoester 4, carrying out alkylation under the condition of sodium ethylate to obtain a compound 5, carrying out a coupling reaction to obtain a compound 6, carrying out an intramolecular olefin double replacement reaction on the compound 6 to obtain a key intermediate compound 7, carrying out reduction with sodium borohydride to obtain a compound 8, carrying out a reaction under the condition of pyridine/MsCl to obtain a compound 9, hydrolyzing the compound 9 under the action of lithium hydroxide, carrying out methyl esterification by using iodomethane to obtain a compound 10, carrying out palladium-carbon catalytic hydrogenation to obtain a pair of diastereoisomers 11 and 12, and carrying out resolution by a semi-preparative high performance liquid chromatograph to obtain the natural product rupestine G and three stereoisomers, namely a compound 13, a compound 14 and a compound 15.