76727-24-7Relevant articles and documents
NOVEL HETEROAROMATIC AMIDE DERIVATIVE AND MEDICINE CONTAINING SAME
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Paragraph 0394; 0397, (2021/07/24)
A compound selectively inhibiting Nav1.7 over Nav1.5 is provided. A heteroaromatic amide derivative or salt thereof showing high efficacy for various diseases associated with Nav1.7 such as pain, represented by the general formula (I) [wherein, X1-X2 is N-C or C-N, Y1 , Y2, Y3 and Y4 are -CH2-, -CR4aH- or -O- and so on, Z1 is-O- and so on, ring A is a 3- to 7-membered monocyclic aromatic ring and so on, R1a and R1b are a hydrogen atom or a halogen atom and so on, R2 is a hydrogen atom and so on, R3a, R3b and R3c are a hydrogen atom or an optionally substituted C1-C6 haloalkyl group and so on, R4a, R4b and R4c are, an optionally substituted C1-C6 haloalkyl group or C1-C6 haloalkoxy group and so on, R5a is a hydrogen atom and so on, R5a and R5b together form -CH2O- and so on, R6a and R6b are a hydrogen atom and so on, n is 1 or 2.].
Synthesis of N-Alkyl Anilines from Arenes via Iron-Promoted Aromatic C-H Amination
Falk, Eric,Gasser, Valentina C. M.,Morandi, Bill
supporting information, p. 1422 - 1426 (2021/03/08)
We report both an intermolecular C-H amination of arenes to access N-methylanilines and an intramolecular variant for the synthesis of tetrahydroquinolines. A newly developed, highly electrophilic aminating reagent was key for the direct synthesis of unprotected N-methylanilines from simple arenes. The reactions display a broad functional group tolerance and employ catalytic amounts of a benign iron salt under mild reaction conditions.
Access to Trisubstituted Fluoroalkenes by Ruthenium-Catalyzed Cross-Metathesis
Nouaille, Augustin,Pannecoucke, Xavier,Poisson, Thomas,Couve-Bonnaire, Samuel
supporting information, p. 2140 - 2147 (2021/03/06)
Although the olefin metathesis reaction is a well-known and powerful strategy to get alkenes, this reaction remained highly challenging with fluororalkenes, especially the Cross-Metathesis (CM) process. Our thought was to find an easy accessible, convenient, reactive and post-functionalizable source of fluoroalkene, that we found as the methyl 2-fluoroacrylate. We reported herein the efficient ruthenium-catalyzed CM reaction of various terminal and internal alkenes with methyl 2-fluoroacrylate giving access, for the first time, to trisubstituted fluoroalkenes stereoselectively. Unprecedent TON for CM involving fluoroalkene, up to 175, have been obtained and the reaction proved to be tolerant and effective with a large range of olefin partners giving fair to high yields in metathesis products. (Figure presented.).