922497-46-9Relevant academic research and scientific papers
Enantio- and chemoselective Br?nsted-acid/Mg(nBu) 2 catalysed reduction of α-keto esters with catecholborane
Enders, Dieter,St?ckel, Bianca A.,Rembiak, Andreas
, p. 4489 - 4491 (2014/04/17)
The first enantio- and chemoselective Br?nsted-acid catalysed reduction of α-keto esters with catecholborane has been developed. The α-hydroxy esters were obtained under mild reaction conditions in virtually quantitative yields and excellent enantioselectivities. With slight modifications both enantiomers can be obtained without any loss of selectivity. This journal is the Partner Organisations 2014.
The preparation of 2H-1,4-benzoxazin-3-(4H)-ones via palladium-catalyzed intramolecular C-O bond formation
Ylijoki, Kai E. O.,Kuendig, E. Peter
supporting information; experimental part, p. 10608 - 10610 (2011/11/05)
Pd/PtBu3-catalyzed intramolecular C-O bond formation has been used to access aryl- and alkyl-substituted benzoxazinones.
Discovery and initial optimization of 5,5′-disubstituted aminohydantoins as potent β-secretase (BACE1) inhibitors
Nowak, Pawel,Cole, Derek C.,Aulabaugh, Ann,Bard, Jonathan,Chopra, Rajiv,Cowling, Rebecca,Fan, Kristi Y.,Hu, Baihua,Jacobsen, Steve,Jani, Minakshi,Jin, Guixan,Lo, Mei-Chu,Malamas, Michael S.,Manas, Eric S.,Narasimhan, Rani,Reinhart, Peter,Robichaud, Albert J.,Stock, Joseph R.,Subrath, Joan,Svenson, Kristine,Turner, Jim,Wagner, Erik,Zhou, Ping,Ellingboe, John W.
scheme or table, p. 632 - 635 (2010/06/12)
8,8-Diphenyl-2,3,4,8-tetrahydroimidazo[1,5-a]pyrimidin-6-amine (1) was identified through HTS, as a weak (micromolar) inhibitor of BACE1. X-Ray crystallographic studies indicate the 2-aminoimidazole ring forms key H-bonding interactions with Asp32 and Asp228 in the catalytic site of BACE1. Lead optimization using structure-based focused libraries led to the identification of low nanomolar BACE1 inhibitors such as 20b with substituents which extend from the S1 to the S3 pocket.
Rigid aminoalcohol backbone as a highly defined chiral template for the preparation of optically active tertiary α-hydroxyl acids
Senanayake, Chris H.,Fang, Kevin,Grover, Paul,Bakale, Roger P.,Vandenbossche, Charles P.,Wald, Stephen A.
, p. 819 - 822 (2007/10/03)
Constrained aminoalcohol derived-ketoester or amides have provided a new entry for the production of enantiopure acid 1 for (S)-oxybutynin.
