- INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE
-
The present invention provides compounds of formula (I): wherein all of the variables are as defined herein. These compounds are inhibitors of indoleamine 2,3-dioxygenase (IDO), which may be used as medicaments for the treatment of proliferative disorders, such as cancer, viral infections and/or autoimmune diseases.
- -
-
Page/Page column 106
(2020/02/16)
-
- Copper-Mediated Oxidative Fluorination of Aryl Stannanes with Fluoride
-
A regiospecific method for the oxidative fluorination of aryl stannanes using tetrabutylammonium triphenyldifluorosilicate (TBAT) and copper(II) triflate is described. This reaction is robust, uses readily available reagents, and proceeds via a stepwise protocol under mild conditions (60 °C, 3.2 h). Broad functional group tolerance, including arenes containing protic and nucleophilic groups, is demonstrated.
- Gamache, Raymond F.,Waldmann, Christopher,Murphy, Jennifer M.
-
supporting information
p. 4522 - 4525
(2016/09/28)
-
- Synthesis and biological activity of some novel substituted quinazoline derivatives
-
A new series of 4-N-(substituted benzyl)-2-phenyl-N-propylquinazolines were synthesized. The structures of the synthesized compounds were confirmed by IR, 1H NMR, 13C NMR and mass spectral analysis. All the synthesized compounds were screened for their analgesic and anti-inflammatory activity. Among the synthesized compounds 5c, 5h and 5o exhibited significant analgesic activity at 60 and 90 minutes reading, while compounds 5g, 5k and 5l exhibited significant anti-inflammatory activity at 3rd and 4th hr reading.
- Srivastav, Maneesh Kumar,Rajeeva,Salahuddin, Md.,Srinivasulu,Shanta Kumar
-
p. 115 - 118
(2019/01/21)
-
- Pd(OAc)2-catalyzed carbonylation of amines
-
A phosphine-free catalytic system [Pd(OAc)2-Cu(OAc) 2-air] induced a substrate-specific carbonylation of amines in boiling toluene under CO gas (1 atm). Symmetrical N,N′-dialkylureas were obtained by the carbonylation of primary amines. N,N,N′-Trialkylureas were selectively formed by addition of a secondary amine to the above reaction vessel. Secondary amines did not give tetraalkylureas. However, dialkylamines with a phenyl group on their alkyl chains, such as N-monoalkylated benzylic amine or phenethylamine derivatives, underwent a direct aromatic carbonylation to afford five- or six-membered benzolactams. In the carbonylation, the chelation effect or steric repulsion between Pd(II) and the meta-substituent in the ortho-palladation and the ring sizes of cyclopalladation products that were formed prior to carbonylation were found to generate good site selectivity and increase the reaction rate. In contrast, carbonylation of ω- arylalkylamines with a hydroxyl group gave neither ureas nor benzolactams but instead produced 1,3-oxazolidinones smoothly. Hydrochlorides of amines also underwent carbonylation to afford the corresponding amides under the conditions used. This procedure made it possible to prepare ureas of amino acid esters and N-alkylcarbamates in practical yields.
- Orito, Kazuhiko,Miyazawa, Mamoru,Nakamura, Takatoshi,Horibata, Akiyoshi,Ushito, Harumi,Nagasaki, Hideo,Yuguchi, Motoki,Yamashita, Satoshi,Yamazaki, Tetsuro,Tokuda, Masao
-
p. 5951 - 5958
(2007/10/03)
-
- Hydroamination of carbonyl compounds with oximes
-
N-alkyl(cycloalkyl)benzylamines, p-fluorobenzylamines, (1-phenylethyl) amines, [1-(p-fluorophenyl)ethyl]amines were synthesized by hydroamination of aldehydes and ketones with oximes.
- Tarasevich,Kozlov
-
p. 379 - 383
(2007/10/03)
-