65169-38-2Relevant articles and documents
Preparation method of Sotorasib intermediate
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Paragraph 0008; 0028-0030; 0034-0036; 0040-0042, (2021/11/06)
The invention discloses a preparation method of a Sotorasib intermediate 2-isopropyl-3-amino-4-methylpyridine. The preparation method comprises the following specific steps of: (1) carrying out a reaction on 3-cyano-4-methyl-2-pyridone and a halogenating reagent to obtain 2-halogenated-3-cyano-4-methylpyridine; (2) making the 2-halogenated-3-cyano-4-methylpyridine with an isopropyl Grignard reagent under the action of a catalyst, so as to obtain 2-isopropyl-3-cyano-4-methylpyridine; (3) carrying out hydrolysis on the 2-isopropyl-3-cyano-4-methylpyridine, so as to obtain 2-isopropyl-4-methyl nicotinamide; and (4) carrying out Hofmann rearrangement on the 2-isopropyl-4-methyl nicotinamide, sodium hydroxide and a sodium hypochlorite solution, so as to obtain the 2-isopropyl-3-amino-4-methylpyridine. The preparation method disclosed by the invention is low in cost and simple to operate, and is a novel method for synthesizing the 2-isopropyl-3-amino-4-methylpyridine.
Method for preparing 2-chloro-4-methylpyridine-3-carbonitrile
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Paragraph 0045; 0051, (2016/11/14)
The invention discloses a method for preparing 2-chloro-4-methylpyridine-3-carbonitrile. The method comprises the following steps: at -20 DEG C to 50 DEG C, a hydrogen chloride solution is used for treating raw materials containing 4,4-dicyano-3-methyl-3-butenal dimethyl acetal. 2-chloro-4-methylpyridine-3-carbonitrile whose HPLC purity reaches 99% or above can be conveniently obtained, which has important meanings for subsequent preparation of high purity 2-chloro-4-methylpyridine-3-carbonitrile and nevirapine; the method has the advantages of short process route, simple operation, high yield, low cost, etc., a highly toxic product phosphorous oxychloride is avoided, discharge of waste water is reduced, and the method is very suitable for industrial production.
HETEROCYCLIC COMPOUNDS AS EP4 RECEPTOR ANTAGONISTS
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Paragraph 0244; 0245, (2016/05/09)
The present invention provides a compound represented by the formula (1): wherein each symbol is as defined in the specification or a salt thereof has an EP4 receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of EP4 receptor associated diseases (e.g., rheumatoid arthritis, aortic aneurysm, endometriosis, ankylosing spondylitis, inflammatory breast cancer etc.) and the like.