Regioselective c2-arylation of imidazo 4 5-b pyridines book

Discovery of 3 h imidazo4,5 b pyridines as potent cmet. Ligandfree coppercatalyzed regioselective c2 arylation. Microwaveassisted c2 direct alkenylation of imidazo4,5 b. We show that n 3memprotected imidazo 4, 5b pyridines undergo efficient c2functionalisation via direct ch arylation. Regioselective c2arylation of imidazo4,5 b pyridines. A facile synthesis of imidazo 4, 5b pyridines and pyrazines is described using a pdcatalyzed amide coupling reaction. Cheminform abstract sp2 sp3 diboranes astounding structural. Agich activation enables nearroomtemperature direct.

Jonathan macdonald, victoria oldfield, vassilios bavetsias, and julian blagg cancer research uk cancer therapeutics unit, division of cancer therapeutics, the institute of cancer. Palladiumcatalyzed regioselective arylation of imidazo1. Palladiumcatalyzed regioselective arylation of imidazo 1,2 b 1,2, 4 triazine. Preliminary mechanistic studies of this arylation are also reported. A model system relevant to the natural product pentosidine has been demonstrated, as well as the total synthesis of the mutagen 1me5phip. Anamik shah vice chancellor, gujarat vidhyapeeth president.

Imidazo 4, 5 b pyridines are an important class of heterocycles that have been widely studied for biological activity. Solventfree synthesis under acidic conditions 267 tetraphenyl porphyrin synthesis 267 acetalization of lgalactono1, 4 lactone 268 aziridine synthesis 268 lactam synthesis 269 arylimidazole synthesis 269 pyridine, pyrazine, and pyridine derivatives 270 quinolines and quinoxalines 271 pyrroles, indoles and related compounds. Incorporation of catalytic pivalic acid as a proton shuttle and a key element in catalyst design. Supplementary information regioselective c2arylation of. This reaction provides quick access to products with substitution at n1 and c2. Another similar study was carried out by doucet and roger in their study of regioselective c2 or c5 arylation using a palladium acetate catalyst. Regioselective substitution of the 6position of 7a or the 7position of 8a by pdmediated crosscoupling see esi schemes s4s7 followed by direct c2arylation gave the desired disubstituted compounds table 5, 16a to 16j. Evidence for a critical role of acetate in the pdoac2 precatalyst. Supplementary information regioselective c2arylation of imidazo 4, 5b pyridines. Regioselective c2arylation of imidazo4,5bpyridines. Rapid construction of an imidazo4,5bpyridine skeleton. This arylation proceeded smoothly without promotion of the ligands, and various functional 22 samples groups were well tolerated. Arylation of pyrroles often occurs with the help of ch activation. An effective, regioselective c2 arylation of imidazo 2,1bthiazoles catalyzed by cui has been developed.

Twentytwo substituted imidazo 4, 5b pyridines are prepared and iterative, selective elaboration of functionalised imidazo 4, 5b pyridines gives 2,7 and 2,6disubstituted derivatives in good yields from common intermediates. Gryko and colleagues demonstrated this in their study of the direct arylation of pyrroles with iodoarenes to form 2arylpyrroles. A facile synthesis of imidazo 4, 5 b pyridines and pyrazines is described using a pdcatalyzed amide coupling reaction. Access to fluorescent purine isosteres with remarkably large stokes shifts we describe herein the first. Twentytwo substituted imidazo 4, 5 b pyridines are prepared and iterative, selective elaboration of functionalised imidazo 4, 5 b pyridines gives 2,7 and 2,6disubstituted derivatives in good yields from common intermediates mechanistic observations are consistent with a.

Institute of cancer research repository items where year is. Regioselective synthesis of c2 substituted imidazo4,5b. Pdf regioselective c2arylation of imidazo4,5bpyridines. We show that n3memprotected imidazo 4, 5b pyridines undergo efficient c2functionalisation via direct ch arylation. Nhydroxy 4 3himidazo 4, 5b pyridin2ylbenzenecarboximidamide was the most active compound with ic50 equal to 0. Csir and gate exams are considered as gate way to do phd in india in various field ranging from biology to engineering,even foreign university expecting students applying from in. Request pdf microwaveassisted c2 direct alkenylation of imidazo 4, 5 b pyridines. Jonathan macdonald, victoria oldfield, vassilios bavetsias, and julian blagg cancer research uk cancer therapeutics unit, division of cancer therapeutics, the institute of cancer research, haddow laboratories, sutton, surrey, sm2 5ng, uk. Supplementary information regioselective c2arylation of imidazo 4, 5 b pyridines. Mechanistic analysis of azine noxide direct arylation. We show that n3memprotected imidazo 4, 5 b pyridines undergo efficient c2functionalisation via direct ch arylation.