62596-18-3Relevant academic research and scientific papers
ATM KINASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF
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Paragraph 0278, (2021/06/11)
Provided are certain ATM kinase inhibitors of Formula (I). Also provided herein are compositions of such compounds, and methods of their use.
Pd(OAc)2-catalyzed carbonylation of amines
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)
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.
Beta 3 agonists. Part 1: Evolution from inception to BMS-194449
Washburn,Sher,Poss,Girotra,McCann,Gavai,Mikkilineni,Mathur,Cheng,Dejneka,Sun,Wang,Harper,Russell,Slusarchyk,Skwish,Allen,Hillyer,Frohlich,Abboa-Offei,Cap,Waldron,George,Tesfamariam,Ciosek Jr.,Ryono,Young,Dickinson,Seymour,Arbeeny,Gregg
, p. 3035 - 3039 (2007/10/03)
Screening of the BMS collection identified 4-hydroxy-3-methylsulfonanilidoethanolamines as full beta 3 agonists. Substitution of the ethanolamine nitrogen with a benzyl group bearing a para hydrogen bond acceptor promoted β3 selectivity. SAR elucidation established that highly selective β3 agonists were generated upon substitution of Cα with either benzyl to form (R)-1,2-diarylethylamines or with aryl to generate 1,1-diarylmethylamines. This latter subset yielded a clinical candidate, BMS-194449 (35).
Cyclic amidino agents useful as nitric oxide synthase inhibitors
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, (2008/06/13)
The current invention discloses useful amidino derivative useful as nitric oxide synthase inhibitors.
