1447607-89-7Relevant articles and documents
Synthesis method of 5-bromine-1-methyl-1H-pyrazole-3-amine
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Paragraph 0016, (2020/12/30)
The invention discloses a synthesis method of 5-bromine-1-methyl-1H-pyrazole-3-amine. The method comprises the steps of condensing diethyl butynedioate serving as a raw material with methylhydrazine to obtain 5-hydroxyl-1-methyl-1H-pyrazole-3-carboxylic acid ethyl ester, and reacting the 5-hydroxyl-1-methyl-1H-pyrazole-3-carboxylic acid ethyl ester with phosphorus oxybromide to obtain 5-bromine-1-methyl-1H-pyrazole-3-carboxylic acid ethyl ester; hydrolyzing in a sodium hydroxide alcohol solution to obtain 5-bromine-1-methyl-1H-pyrazole-3-carboxylic acid, reacting the 5-bromine-1-methyl-1H-pyrazole-3-carboxylic acid with dimethyl azide phosphate and tert-butyl alcohol to obtain tert-butyl (5-bromine-1-methyl-1H-pyrazole-3-yl) carbamate, and hydrolyzing in trifluoroacetic acid to obtain the5-bromine-1-methyl-1H-pyrazole-3-amine. The method has the advantages of simple synthesis route, reasonable process selection, low raw material cost, simple and easily available raw materials, convenient operation and post-treatment, and no use of highly toxic reagents, and overcomes the defects of expensive and unavailable raw materials, unsafe operation, difficult amplification and the like in the existing synthesis process.
MACROCYCLIC AZOLOPYRIDINE DERIVATIVES AS EED AND PRC2 MODULATORS
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Paragraph 1017; 1030, (2020/10/09)
The invention relates to modulators of Embryonic Ectoderm Development (EED) and/or Polycomb Repressive Complex 2 (PRC2) useful in the treatment of disorders and diseases associated with EEC and PRC2, being macrocyclic azolopyridine derivatives and compositions thereof of Formula (I), or a pharmaceutically acceptable salt, prodrug, solvate, hydrate, enantiomer, isomer, or tautomer thereof, wherein X1, X2, X3, A1, A2, Y, R1, R2, R3, and R4 are as described herein.