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.
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.
LOWCOST, HIGH YIELD SYNTHESIS OF NEVIRAPINE
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Page/Page column 23; 24, (2016/12/22)
Improved methods of producing the HIV drug substance, nevirapine are provided. The methods employ a cost effective and high yield synthetic methods for preparing the nevirapine building block 2-chloro-3-amino-4-picoline (CAPIC) and 2-cyclopropyl amino nicotinate (Me-CAN), and improvements in other steps of nevirapine synthesis.