1221722-10-6Relevant articles and documents
Large-steric-hindrance N-heterocyclic carbene palladium complex, preparation method and application thereof, and synthesis method of sonidegib based on large-steric-hindrance N-heterocyclic carbene palladium complex
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Paragraph 0136; 0138-0141, (2021/01/24)
The invention belongs to the technical field of organic synthesis and chemical catalysis, and discloses a large-steric-hindrance N-heterocyclic carbene palladium complex, a preparation method thereof,an application of the complex in efficient catalysis of a C-N coupling reaction under a room-temperature air condition, and a synthesis method of sonidegib based on the complex. According to the large-steric-hindrance N-heterocyclic carbene palladium complex, diphenyl imidazole serves as a main ligand framework, functionalized allyl serves as an auxiliary ligand, the functionalized allyl is introduced beside a metal center of a catalyst to serve as an auxiliary ligand, the catalytic activity and stability are remarkably improved, the large-steric-hindrance N-heterocyclic carbene palladium complex can be applied to efficient catalysis of a CN coupling reaction, particularly, the CN coupling reaction can be efficiently catalyzed under the room temperature condition, and the yield can reachup to 99%. The invention also provides a method for synthesizing sonidegib by taking aryl/aliphatic amine and aryl chloride as reactants and a three-step method at room temperature under the catalysisof a palladium catalytic system, the synthetic method has few steps, and the total yield can reach 74.5%.
PROCESS FOR THE PREPARATION OF N-[6-(CIS-2,6-DIMETHYLMORPHOLIN-4-YL)PYRIDINE-3-YL]-2- METHYL-4'-(TRIFIUOROMETHOXY) [1,1' -BIPHENYI]-3-CARBOXAMIDE AND ITS POLYMORPHS THEREOF
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Page/Page column 48, (2017/10/30)
The present invention relates to process for the preparation of N-[6-(cis-2,6-dimethyl morpholin-4-yl)pyridine-3-yl]-2-methyl-4' -(trifluoromethoxy) [1,1'-biphenyl]-3-carboxamide compound of formula-1, it's salts and their polymorphs thereof.
METABOLITES OF SONIDEGIB (LDE225)
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Page/Page column 18; 19, (2015/07/07)
Provided herein are metabolites of N-(6-((2R,6S)-2,6-dimethylmorpholino)pyridin-3-yl)- 2-methyl-4'-(trifluoromethoxy)-[1,1'-biphenyl]-3-carboxamide (Sonidegib, LDE225) that modulate the activity of the Hedgehog signaling pathway and that are useful in the