78781-84-7Relevant academic research and scientific papers
GRANZYME B DIRECTED IMAGING AND THERAPY
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Page/Page column 115-116, (2019/09/04)
Provided herein are heterocyclic compounds useful for imaging Granzyme B. Methods of imaging Granzyme B, combination therapies, and kits comprising the Granzyme B imaging agents are also provided.
CYSTEINE PROTEASE INHIBITORS
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, (2011/06/26)
Compounds of the formula (I) wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and Rs
Impact on hydrogenation catalytic cycle of the R groups Cyclic feature in "r-SMS-Phos"
Zupancic, Borut,Mohar, Barbara,Stephan, Michel
supporting information; experimental part, p. 3022 - 3025 (2010/08/19)
A series of R-SMS-Phos ligands was evaluated in the Rh(I)-catalyzed hydrogenation of a set of olefins showing a marked influence of the cyclic nature and structure of the R groups. Overall, cPen- and Cy-SMS-Phos performed efficiently, while Ph- and Bn-SMS-Phos exhibited slower kinetics and furnished lower ees also compared with C6F5CH2-SMS-Phos. The Rh(I)-(Cy-SMS-Phos) catalyst was screened under mild conditions displaying excellent enantioselectivities and high TOFs. Cases of catalysis under catalyst or substrate control were identified.
Facile asymmetric synthesis of α-amino acids employing chiral ligand-mediated asymmetric addition reactions of phenyllithium with imines
Hasegawa, Masayoshi,Taniyama, Daisuke,Tomioka, Kiyoshi
, p. 10153 - 10158 (2007/10/03)
A three-step methodology involving an external chiral ligand-mediated asymmetric addition of phenyllithium to an anisidine imine, oxidative removal of N-PMP group, and finally oxidative conversion of the phenyl group to a carboxyl group provides a facile synthesis of optically pure α-amino acid derivatives beating a bulky α-substituent. (C) 2000 Elsevier Science Ltd.
Efficient chemoenzymatic synthesis of enantiomerically pure α-amino acids
Beller, Matthias,Eckert, Markus,Geissler, Holger,Napierski, Bernd,Rebenstock, Heinz-Peter,Holla, E. Wolfgang
, p. 935 - 941 (2007/10/03)
A general two-step chemoenzymatic synthesis for enantiomerically pure natural and nonnatural α-amino acids is presented. In the first step of the sequence, the ubiquitous educts aldehyde, amide and carbon monoxide react by palladium-catalyzed amidocarbonylation to afford the racemic N-acyl amino acids in excellent yields. In the second step, enzymatic enantioselective hydrolysis yields the free optically pure a-amino acid and the other enantiomer as the N-acyl derivative, both in optical purities of 85-99.5% ee. The advantage of the chemoenzymatic process compared to other amino acid synthesis are demonstrated by the preparation of various functionalized (-OR, -Cl, -F, -SR) α-amino acids on a 10-g scale.
On Amino Acid Antagonists,IV.-Separation and Determination of the Configurations of the Stereoisomeric N-Acetyl-2-(2'-cyclohexenyl)glycines
Santoso, Sentot,Kemmer, Thorsten,Trowitzsch, Wolfram
, p. 642 - 657 (2007/10/02)
The D-(+)-(1-phenylethyl)amides 5 as well as the D-(-)-O-acetyl-α-phenylglycinolamides 7 of the title compounds were separated on silica gel into the four diastereomeric compounds.All attempts failed to hydrolyze 5 and 7 to the corresponding acids.In contrast the diastereomeric D-(-)-N-acetyl-α-phenylglycinol esters 10 which were separated on silica gel were hydrolysed to the optically active acids 3a-d.The absolute configurations at C-2 in 3 were determined by correlation with the saturated glycine derivatives of known stereochemistry.The relative configurationsand hence the absolute configurations at C-1' in 3a-d were deduced from the NMR- and CD-spectra and were confirmed by X-ray analysis of 3a.Only the amino acid 3b with the (2S,1'R)-configuration exhibits biological activity.
