59938-06-6Relevant articles and documents
Regioselective synthesis of 2-acetyl- and 2-alkoxycarbonyl-3- (trifluoromethyl)phenols by [3+3] cyclization of 1,3-bis-silyl enol ethers with 4-ethoxy- and 4-silyloxy-1,1,1-trifluoroalk-3-en-2-ones
Mamat, Constantin,Pundt, Thomas,Schmidt, Andreas,Langer, Peter
, p. 2183 - 2185 (2006)
2-Acetyl- and 2-alkoxycarbonyl-3-(trifluoromethyl)phenols were prepared by [3+3] cyclization of 1,3-bis-silyl enol ethers with 4-ethoxy- and 4-silyloxy-1,1,1-trifluoroalk-3-en-2-ones.
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Gambaryan,N.P. et al.
, (1967)
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KRAS G12C Mutant protein inhibitor and pharmaceutical composition thereof Preparation method and application
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Paragraph 0191; 0193; 0197-0199, (2021/10/27)
The present invention provides compounds having irreversible inhibitor activity G12C mutant KRAS protein, racemates, stereoisomers, pharmaceutically acceptable salts, polymorphs or solvates thereof, the structure of which is shown in formula (I). Also provided are methods related to the preparation and use of such compounds, pharmaceutical compositions comprising such compounds, and methods of modulating G12C mutant KRAS protein activity for treatment of disorders such as cancer.
Preparation process 4 - trifluoromethyl nicotinic acid
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Paragraph 0021-0022; 0027-0028; 0033-0034; 0039-0040, (2021/10/11)
The invention discloses a preparation process of 4 -trifluoromethyl nicotinic acid and vinyl ether. Trifluoracetyl chloride and catalyst were added to the reactor and stirred. Acylation to obtain 4 - ethoxy -1, 1, 1 -trifluoro -3 - alkene -2 - ketone, reacting 4 - with a catalyst and an oxidizing agent to -1 ethoxy 1, 1 -3 -trifluoro -2 -butenone, 25 - 90 °C g 30 - 60min of 1-trifluoroethyl 1-butenecone, adding 1 - equivalents of alkali lye, and then acidifying to obtain -4 - 2-trifluoromethylnicotiniconicotinic acid, followed by acidification with -3 - 4 -chloro 1 - 5-4 - trifluoromethyl POCl3 picolinic 6 - acid -4 . The preparation method of 4 -trifluoromethyl nicotinic acid is optimized. Only the reaction temperature is controlled, the intermediate product can be used for subsequent reaction steps, the reaction requirements in the step process are reduced, the requirement for equipment is low, and industrialization can be conveniently realized.
Preparation method of N-(2-methoxycarbonyl vinyl)-4, 4, 4-trifluoro-3-ketone-1-buteneamine
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Paragraph 0017; 0020; 0023; 0026; 0029; 0032; 0035; 0038, (2021/07/17)
The invention belongs to the technical field of medicine synthesis, and particularly relates to a preparation method of N-(2-methoxycarbonyl vinyl)-4, 4, 4-trifluoro-3-ketone-1-buteneamine, and the preparation method of N-(2-methoxycarbonyl vinyl)-4, 4, 4-trifluoro-3-ketone-1-buteneamine comprises the following steps: taking trifluoroacetic acid, vinyl ethyl ether, methylsulfonyl chloride and pyridine as raw materials, firstly preparing 4-ethoxy-1, 1, 1-trifluoro-3-butene-2-ketone, carrying out ammonia ammoniation to obtain 4-amino-1, 1, 1-trifluoro-3-butene-2-ketone, then, under the action of sodium hydroxide, reacting with methyl 3-methoxyacrylate to obtain a target product N-(2-methoxycarbonyl vinyl)-4, 4, 4-trifluoro-3-ketone-1-buteneamine. The adopted raw materials are relatively cheap and easy to obtain, and the method is easy and convenient to operate, safe, feasible, high in cost performance and suitable for industrial production.