- Double head-to-tail direct arylation as a viable strategy towards the synthesis of the aza-analog of dihydrocyclopenta[hi]aceanthrylene-an intriguing antiaromatic heterocycle
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The first case of double head-to-tail direct arylation of aromatic compounds and the unusual photophysical properties of the resulting 2,2a1,5b1,7-tetraazacyclopenta[hi]aceanthrylene are reported. This molecule, comprising of two imidazo[1,2-a]pyridine units, is antiaromatic due to the changes in the efficiency of π-electron ring current and it belongs to a class of seldom encountered compounds with a dark lowest electronically excited singlet state.
- Firmansyah, Dikhi,Deperasińska, Irena,Vakuliuk, Olena,Banasiewicz, Marzena,Tasior, Mariusz,Makarewicz, Artur,Cyrański, Micha? K.,Kozankiewicz, Boles?aw,Gryko, Daniel T.
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- METALLO-BETA-LACTAMASE INHIBITORS
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The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
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Page/Page column 85; 86
(2017/04/04)
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- IMIDAZO[1,2-A]PYRIDINE AND PYRAZOLO[2,3-A]PYRIDINE DERIVATIVES
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A compound of formula (I) wherein Ring A is imidazol[1,2a]pyrid-3-yl or pyrazolo[2,3a]pyrid-3-yl; Ris as defined within; m is 0-5; wherein the values of Rmay be the same or different; Ris as defined within; n is 0 to 2, wherein the values of Rmay be the same or different; Ring B is phenyl or phenyl fused to a C5-7cycloalkyl ring; Ris as defined within; p is 0-4; wherein the values of Rmay be the same or different; Ris as defined within; q is 0-2; wherein the values of Rmay be the same or different; and wherein p+q=5; or a pharmaceutically acceptable salt or an in vivo hydrolyzable ester thereof is described. The use of compounds of formula (I) in the inhibition of cell cycle kinases CDK2, CDK4, and CDK6 are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.
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Page/Page column 38
(2010/02/04)
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- KINASE INHIBITORS
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The present invention provides kinase inhibitors of Formula (I)
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Page/Page column 20
(2010/02/07)
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- PURINE DERIVATIVES AS KINASE INHIBITORS
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The present invention provides kinase inhibitors of Formula I.
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Page/Page column 40
(2008/06/13)
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- peri-Substituted Imidazopyridines. A New Reductive Elimination Reaction
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A new reductive elimination reaction of 3,5-disubstituted imidazopyridines (3) with hydrazine is reported.Thus on treatment of the 3,5-dibromo (7a), 5-bromo-3-nitro (7b), and 3,5-dinitro (4) derivatives with hydrazine hydrate in hot ethanol, the bromine and nitro groups are replaced by hydrogen.A mechanism based on the conjugated relationship of these peri-substituents is proposed and used to explain the reported conversion of 1,3,5-trichloro-2,4,6-trinitrobenzene (9) into 1,3-dichloro-4,6-dinitrobenzene (10).A variety of other 3-nitro-5-substituted imidazopyridines (15)-(18) is described, but these could not be cyclised to 1,2,4-triazacyclopentindenes.The 3-amino-5-methoxycarbonyl derivative (19a) cyclises to the triazacyclopentindenone (20) with sodium methoxide.
- Rees, Charles W.,Smith, David I.
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p. 1159 - 1164
(2007/10/02)
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