- Preparation method of 3-fluoro-4-trifluoromethyl cyanophenyl
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The invention discloses a preparation method of 3-fluoro-4-trifluoromethyl cyanophenyl, which comprises the following steps of dissolving 2-chloro-3-fluoro-4-trifluoromethyl benzaldehyde and hydroxylamine salt in a first solvent, then adding a first acid-binding agent, heating to 60-180 DEG C, and reacting for 2-4 hours to obtain 2-chloro-3-fluoro-4-trifluoromethyl cyanophenyl, and dissolving the 2-chloro-3-fluoro-4-trifluoromethyl cyanophenyl and a second acid-binding agent in a second solvent, adding a catalyst, carrying out hydrogen displacement, carrying out a stirring reaction at 0-180 DEG C under the hydrogen pressure of 0.1-1 MPa for 4-8 h, and cooling to 0-5 DEG C to obtain the 3-fluoro-4-trifluoromethyl cyanophenyl. The product yield reaches 85% or above, the purity is 95% or above, the reaction operation is simple, the generated three wastes are few, and the method has a good industrial prospect.
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Paragraph 0026; 0029; 0030; 0033; 0034; 0037; 0038; 0041
(2021/06/22)
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- A novel and convenient synthesis of benzonitriles: Electrophilic cyanation of aryl and heteroaryl bromides
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N-Cyano-N-phenyl-p-methylbenzenesulfonamide has been used as a more benign electrophilic cyanation reagent for the synthesis of various benzonitriles from (hetero)aryl bromides via formation of Grignard reagents. Electronically different and sterically demanding aryl bromides including functionalized substrates and heteroaryl bromides are successfully cyanated in good to excellent yields. The efficiency of the present methodology is shown by the expeditious syntheses of interesting pharmaceutical intermediates. Notably, chemoselective monocyanation of dibromoarenes is also achieved. Copyright
- Anbarasan, Pazhamalai,Neumann, Helfried,Beller, Matthias
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supporting information; experimental part
p. 4217 - 4222
(2011/05/06)
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- PYRIDO[3,4-D]PYRIMIDINYL ACETAMIDE DERIVATIVES AS TRPA1 MODULATORS
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Provided are pyrido[3,4-d]pyrimidinyl acetamide derivatives as Transient Receptor Potential Ankyrin (TRPA) modulators. In particular, the compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by Transient Receptor Potential Ankyrin 1 (TRPAl). Also provided herein are processes for preparing the compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. Formula (I).
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Page/Page column 23
(2011/11/06)
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