69555-16-4Relevant articles and documents
Isoform-selective thiazolo[5,4-b]pyridine S1P1 agonists possessing acyclic amino carboxylate head-groups
Reed, Anthony B.,Lanman, Brian A.,Neira, Susana,Harrington, Paul E.,Sham, Kelvin K.C.,Frohn, Mike,Pickrell, Alexander J.,Tasker, Andrew S.,Gore, Anu,Fiorino, Mike,Itano, Andrea,McElvain, Michele,Middleton, Scot,Morrison, Henry,Xu, Han,Xu, Yang,Wong, Min,Cee, Victor J.
supporting information; experimental part, p. 1779 - 1783 (2012/04/04)
Replacement of the azetidine carboxylate of an S1P1 agonist development candidate, AMG 369, with a range of acyclic head-groups led to the identification of a novel, S1P3-sparing S1P1 agonist, (-)-2-amino -4-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo[5,4-b]pyridin-2-yl) phenyl)-2-methylbutanoic acid (8c), which possessed good in vivo efficacy and pharmacokinetic properties. A 0.3 mg/kg oral dose of 8c produced a statistically significant reduction in blood lymphocyte counts 24 h post-dosing in female Lewis rats.
Palladium catalysed asymmetric alkylation of benzophenone Schiff base glycine esters in ionic liquids
Kim, Dae Hyun,Im, Jin Kyu,Kim, Dae Won,Cheong, Minserk,Kim, Hoon Sik,Mukherjee, Deb Kumar
experimental part, p. 467 - 476 (2012/03/26)
Asymmetric alkyl substitution of various benzophenone Schiff base substrates under biphasic conditions proceeded using optically active Palladium(II) complexes. The corresponding products were obtained in high yields but with moderate enantiomeric excess (ee) . Addition of specific ionic liquids to the reaction medium enhanced reactivity and selectivity for phase transfer catalytic (PTC) glycine alkylation. It has been found that there is an anionic influence of the ionic liquids that modify the steric environment around the enolate ion. A computer-assisted molecular design of enantioselective phase-transfer catalysis with the palladium complex and the ionic liquid has been done. Indian Academy of Sciences.
Easy and efficient generation of reactive anions with free and supported ylides as neutral Bronsted bases
Palacios, Francisco,Aparicio, Domitila,De Los Santos, Jesús M.,Baceiredo, Antoine,Bertrand, Guy
, p. 663 - 669 (2007/10/03)
The tris(dimethylamino)-C-dimethylphosphorus ylide 5 and the tris(dimethylamino)phosphorus ylide C-bound to Merrifield's resin 6 are used as strong non-nucleophilic bases in N-alkylation reactions of β-amino phosphine oxides and α-amino acid derivatives,