168292-71-5Relevant articles and documents
THERAPEUTIC COMPOUNDS
-
Page/Page column 32, (2017/08/22)
The present invention relates to compounds that are antagonists of the orexin-1 receptor. The compounds have the structural formula (I) defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or disorders associated with orexin-1 receptor activity.
Synthesis of aromatic α-aminoesters: Palladium-catalyzed long-range arylation of primary Csp3-H bonds
Aspin, Sam,Goutierre, Anne-Sophie,Larini, Paolo,Jazzar, Rodolphe,Baudoin, Olivier
, p. 10808 - 10811 (2013/01/15)
Remote control: The title reaction for β-Iζ arylation of α-amino esters with aryl bromides is described. This reaction, which occurs selectively at the terminal position of linear alkyl chains, gives rise to synthetically useful (hetero)arylalanines and homologues after debenzylation (see scheme). Copyright
'N-stereogenic quaternary ammonium salts' from L-amino acids: Synthesis, separation, and absolute configuration
Wu, Hua-Fang,Lin, Wen-Bin,Xia, Li-Zi,Luo, Ying-Gang,Chen, Xiao-Zhen,Li, Guo-You,Zhang, Guo-Lin,Pan, Xin-Fu
experimental part, p. 677 - 688 (2009/08/08)
Diastereoisomeric linear and cyclic 'N-chiral quaternary ammonium salts' (QASs) were efficiently synthesized from corresponding L-amino acids in high yields. The diastereoisomers of each pair of 'N-chiral QASs' were successfully separated. The absolute configurations of these QASs were determined predominately by X-ray single-crystal analysis. The 1H-NMR data of 'N-chiral QASs' provided characteristic information on the configuration of the N-chiral center. 'N-Chiral QASs' exemplified by [N(R)]-2a and [N(S)]-2a are stable in protic and aprotic solvents within a broad pH and temperature range.
Photoinduced electron transfer (PET) promoted oxidative activation of 1- (N-benzyl-N-methylglycyl)-(S)-prolinol: Development of novel strategies towards enantioselective syntheses of α-amino acids, their N-methyl derivatives and α-hydroxy acids employing
Pandey, Ganash,Das, Parthasarathi,Reddy, P. Yella
, p. 657 - 664 (2007/10/03)
PET activation of 1-(N-benzyl-N-methylglycyl)-(S)-prolinol (1) in dry acetonitrile, utilizing 1,4-dicyanonaphthalene (DCN) as a light-harvesting electron-acceptor and methyl viologen (MV++) as an electron-transfer mediator, leads to the formati
Chirale Boran-Amin-Addukte in der asymmetrischen Synthese: Alkylierung von Alaninderivaten
Ferey, Vincent,Toupet, Loic,Gall, Thierry Le,Mioskowski, Charles
, p. 475 - 477 (2007/10/03)
Keywords: Aminosaeuren; Asymmetrische Synthesen; Borverbindungen; Chiralitaet; Enolate
Synthesis and utilization of a novel glycine derived chiral precursor, based on a recyclable L-prolinol auxiliary, for the enantioselective preparation of α-amino acids and their N-methyl derivatives
Pandey,Reddy,Das
, p. 3175 - 3178 (2007/10/03)
α-Amino acids and their N-methyl derivatives are synthesized in fairly high optical purity employing a new glycine derived template based on a recyclable L-prolinol chiral auxiliary.
Stereospecific Amination by Dynamic Kinetic Resolution Utilizing 2-Oxoimidazolidine-4-carboxylate as a Novel Chiral Auxiliary
Kubota, Hitoshi,Kubo, Akira,Takahashi, Masami,Shimizu, Ryo,Da-te, Tadamasa,et al.
, p. 6776 - 6784 (2007/10/03)
A novel type of stereospecific amination by dynamic kinetic resolution using (4S)-2-oxoimidazolidine-4-carboxylate (1) as a chiral auxiliary was developed. A reaction of a diastereomeric mixture of (4S)-3--2-oxoimidazolidine-4-carboxylates 4 with an amine in the presence of a base in HMPA predominantly afforded (4S)-3--2-oxoimidazolidine-4-carboxylates (S,R)-7 in good yields.The reaction proceeded by stereospecific SN2 type amination incorporated with rapid interconversion between the substrates (S,S)-4 and (S,R)-4.Mechanistic study suggested that the unique stereoselectivity was induced through the interaction between an amine and the ester group of (S,S)-4 in the transition state.The chiral auxiliary was easily removed with alkoxide anion to afford the α-amino acid synthon in good yields.
