52648-77-8Relevant articles and documents
Palladium(II)-Catalyzed C(sp2)-H Bond Activation/C-N Bond Cleavage Annulation of N-Methoxy Amides and Arynes
Cheng, Xiu-Fen,Yu, Ting,Liu, Yi,Wang, Nan,Chen, Zhenzhen,Zhang, Guang-Lu,Tong, Lili,Tang, Bo
supporting information, p. 2087 - 2092 (2022/04/07)
The Pd(II)-catalyzed C-H bond activation/C-N bond cleavage annulation reaction of N-alkyoxyamide aryne is developed to synthesize 9,10-dihydrophenanthrenone derivatives. This reaction exhibited good functional group compatibility with yields up to 92%. Detailed mechanistic studies showed that the key to C-N bond cleavage is the formed eight-membered palladacycle intermediate undergoing nucleophilic addition to the carbonyl group, which provides a new and practical way for N-alkoxyamide directed C-H bond activation.
INHIBITORS OF C-FMS KINASE
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Page/Page column 33, (2008/06/13)
The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, es
1,1-DISUBSTITUTED CYCLOALKYL DERIVATIVES AS FACTOR XA INHIBITORS
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Page 236-237, (2010/02/05)
The present application describes 1,1-disubstituted cycloalkyl compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
Thermal Decomposition of
Wolf, Richard A.,Trocino, Richard J.,Rozich, William R.,Sabeta, Isidore C.,Ordway Jr., Richard J.
, p. 3814 - 3820 (2007/10/03)
A series of tert-butyl 1-arylcycloalkyl peresters was prepared, and the rate constants for the peresters' thermal decomposition were measured at several temperatures. The decomposition rates and aryl-substituent effects on the decomposition rates for the three series of peresters are remarkably similar to each other and to the acyclic α,α-dimethylbenzyl analogue previously investigated. The magnitude of the activation parameters for the rates of thermolysis of the alicyclic peresters and the solvent viscosity effects on these rates suggest that the 1-arylcyclobutyl (2), -cyclopentyl (3), and -cyclohexyl (4) peresters undergo thermal decomposition primarily by the concerted, two-bond-cleavage mechanism and that the 1-arylcyclopropyl peresters (1) undergo thermolysis primarily by the stepwise mechanism.
Synthesis of a potential M1 muscarinic agent [76Br] bromocaramiphen
Strijckmans,Hunter,Dolle,Coulon,Loc'h,Maziere
, p. 471 - 481 (2007/10/03)
[76Br]bromocaramiphen was prepared from the iodo-analogue by a Cu+ nucleophilic bromodeiodination exchange. The radiolabelling yield was 40-45%. The radiochemical and chemical purities assessed by radio-TLC and HPLC were 98%. The precursor, iodocaramiphen, was synthesized from commercially available 1-phenylcyclopentanecarboxylic acid with a 10% overall yield in a 5 step procedure. This synthesis includes the formation of 1-(p-nitrophenyl)-, 1-(p-aminophenyl)- and 1-(p-iodophenyl) cyclopemane carboxylic acid. In vivo studies in rats showed high uptake in brain. A 10% decrease was observed by coinjecting with the radiotracer a cold load of QNB, a non subtype selective muscarinic ligand. The metabolite study performed in the pons tissues indicated that there was still 92% of unchanged radiotracer 30 mm p.i. After coinjection of dextrometorphan, a sigma ligand, a reduction of the radioactivity uptake by 20 to 27% was observed in the pons, the cortex, the striatum and the cerebellum. These data suggest that [76Br]bromocaramiphen is not a potential probe for investigating the status of central M1 muscarinic receptors because of its high lipophilicity (log P7 4 = 2.4) and its affinity for sigma sites.
