33691-09-7Relevant academic research and scientific papers
PROCESSES FOR THE PREPARATION OF PYRIMIDINYLCYCLOPENTANE COMPOUNDS
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Page/Page column 42, (2015/06/03)
The present invention relates to a process for the preparation of a compound of formula (I), wherein R1 is as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.
An efficient catalytic asymmetric synthesis of a β2-amino acid on multikilogram scale
Remarchuk, Travis,Babu, Srinivasan,Stults, Jeffrey,Zanotti-Gerosa, Antonio,Roseblade, Stephen,Yang, Shaohui,Huang, Ping,Sha, Chunbo,Wang, Youchu
supporting information, p. 135 - 141 (2014/05/20)
We describe herein a scalable catalytic asymmetric hydrogenation process for the multikilogram-scale production of a β 2-amino acid. A short and efficient synthesis of the starting unsaturated N-Boc-protected β 2-enamide was developed followed by extensive catalysis screening and optimization studies that identified a simple Ru-BINAP catalyst system to directly afford the (S) product in high enantiomeric excess and yield. The final process enabled the multikilogram production in >99% ee, to be used as a key component for one of our clinical candidates.
Lewis base catalyzed asymmetric hydrosilylation of α-substituted β-enamino esters: Facile access to enantioenriched β2-amino esters via dynamic kinetic resolution
Shu, Chang,Hu, Xiao-Yan,Li, Shuai-Shuai,Yuan, Wei-Cheng,Zhang, Xiao-Mei
supporting information, p. 1879 - 1882 (2014/08/18)
A chiral Lewis base organocatalyzed asymmetric hydrosilylation of α-substituted β-enamino esters is presented. The reactions proceeded through dynamic kinetic resolution to afford various enantioenriched β2-amino esters with high yields (up to
PROCESS FOR MAKING AMINO ACID COMPOUNDS
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Paragraph 0086, (2013/12/03)
The invention provides new processes for making and purifying amino acid compounds, which are useful in the preparation of AKT inhibitors used in the treatment of diseases such as cancer, including the compound (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.
Discovery of isoxazolinone antibacterial agents. Nitrogen as a replacement for the stereogenic center found in oxazolidinone antibacterials
Snyder, Lawrence B.,Meng, Zhaoxing,Mate, Robert,D'Andrea, Stanley V.,Marinier, Anne,Quesnelle, Claude A.,Gill, Patrice,Den Bleyker, Kenneth L.,Fung-Tomc, Joan C.,Frosco, MaryBeth,Martel, Alain,Barrett, John F.,Bronson, Joanne J.
, p. 4735 - 4739 (2007/10/03)
A series of potential antimicrobial derivatives possessing bioisosteric replacements for the central oxazolidinone ring found in oxazolidinone antibacterials have been prepared. The design concept involved replacement of the requisite sp3-hybridized stereogenic center found at the 5-position of the oxazolidinone with a nitrogen atom. The synthesis and antibacterial activity of three such ring systems, the benzisoxazolinones, pyrroles, and isoxazolinones is described.
Structure-activity relationships of the peptide deformylase inhibitor BB-3497: Modification of the methylene spacer and the P1′ side chain
Davies, Stephen J.,Ayscough, Andrew P.,Beckett, R. Paul,Bragg, Ryan A.,Clements, John M.,Doel, Sheila,Grew, Christine,Launchbury, Steven B.,Perkins, Gemma M.,Pratt, Lisa M.,Smith, Helen K.,Spavold, Zoe M.,Thomas, S. Wayne,Todd, Richard S.,Whittaker, Mark
, p. 2709 - 2713 (2007/10/03)
Structural modifications to the peptide deformylase inhibitor BB-3497 are described. In this paper, we describe the initial SAR around this lead for modifications to the methylene spacer and the P1′ side chain. Enzyme inhibition and antibacterial activity data revealed that the optimum distance between the N-formyl hydroxylamine metal binding group and the P1′ side chain is one unsubstituted methylene unit. Additionally, lipophilic P1′ side chains that closely mimic the methionine residue in the substrate provided compounds with the best microbiological profile.
Pyrimidin-4-one derivatives, their intermediates for their production and processes for producing these compounds
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, (2008/06/13)
PCT No. PCT/JP96/02169 Sec. 371 Date Feb. 10, 1998 Sec. 102(e) Date Feb. 10, 1998 PCT Filed Aug. 1, 1996 PCT Pub. No. WO97/06150 PCT Pub. Date Feb. 20, 1997Novel pyrimidin-4-one derivatives of formula [1] are provided, which are useful as active ingredien
1(2H)-Isoquinolone compounds and acid addition salts thereof
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, (2008/06/13)
1(2H)-Isoquinolone compounds represented by the formula (1) STR1 wherein Y represents hydrogen, chlorine or a methoxy group, Z represents a straight chain or branched chain divalent saturated aliphatic hydrocarbon group having 2 to 4 carbon atoms, R1
