On June 15, 2016, Wang, Guangyong; Li, Chaoping; Zhou, Zhiguo; Gao, Qiang; Zheng, Baofu published a patent.Name: Methyl 2-methyl-1H-indole-3-carboxylate The title of the patent was Synthetic method of histone methylation enzyme EZH2 inhibitor intermediate. And the patent contained the following:
The invention relates to the synthetic method of histone methylation enzyme EZH2 inhibitor intermediate. The title synthetic method includes (1) mixing compound 1 (Z is NH, NBoc, O, etc.) with reducing agent ((R)-MeCBS-borane dimethylsulfide, sodium borohydride, etc.) in solvent (methanol, ethanol, etc.) at (-10)-0°C, stirring at 0-5°C for 10 min, quenching with hydrochloric acid at (-5)-0°C, adding Me tert-Bu ether, stirring, filtering, layering, extracting water phase with Me tert-Bu ether, collecting organic phase, washing with saturated brine, drying, filtering, and concentrating to obtain compound 2; (2) reacting with methanesulfonyl chloride in presence of base (triethylamine, N,N-diisopropylethylamine, etc.) to obtain compound 3; (3) performing nucleophilic substitution reaction with compound 4 in organic solvent (N,N-dimethylformamide, N,N-dimethylaniline, etc.) in presence of base (sodium hydrogen, sodium carbonate, etc.) at 80-130°C to obtain compound 5; and (4) performing hydrolysis. The preparation method has high product yield, simple process, convenient post treatment, readily available raw materials and environment friendliness. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Name: Methyl 2-methyl-1H-indole-3-carboxylate
The Article related to acetyl heterocycloalkane asym reduction, hydroxy ethyl heterocycloalkane stereoselective preparation methanesulfonylation, mesylate preparation indolecarboxylate nucleophilic substitution hydrolysis, histone methylation enzyme ezh2 inhibitor intermediate preparation green chem and other aspects.Name: Methyl 2-methyl-1H-indole-3-carboxylate
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Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles