76932-17-7Relevant academic research and scientific papers
Ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenylpropanoate], processes for its preparation and its use
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Page/Page column 3; 7, (2008/06/13)
The present invention relates to ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate], the preparation of ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate] from (2R)-2-bromo-3-phenylpropionic acid and ethylenediamine in 2-propanol, and the use of ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate] for the preparation of ACE/NEP inhibitors.
Crystallization-induced chiral inversion as the key step for synthesis of (S)-2-acetylthio-3-phenylpropanoic acid from L-phenylalanine
Chen, Jason G.,Zhu, Jingyang,Skonezny, Paul M.,Rosso, Victor,Venit, John J.
, p. 3233 - 3235 (2007/10/03)
(Chemical Equation Presented) A novel crystallization-induced chiral inversion of (S)-2-bromo-3-phenylpropanoic acid to its (R)-enantiomer with excellent enantiomeric excess (96-99%) is achieved. Optically pure (S)-2-acetylthio-3-phenylpropanoic acid can
Design and synthesis of chromogenic thiopeptolide substrates as MetAPs active site probes
Cui, Yong-Mei,Li, Jing-Ya,Chen, Ling-Ling,Li, Jia,Ye, Qi-Zhuang,Nan, Fa-Jun
, p. 2853 - 2861 (2007/10/03)
Twenty one chromogenic thiopeptolide substrates were designed and synthesized as the active site probes and analyzed with each S1 site of mutant residues and enzymes of wild-type MetAP1s. The preliminary enzymatic experiments indicate that cysteine 70 or 202, at either Escherichia coli or human MetAP1, played a crucial role in the methionine hydrolysis.
PROCESS FOR PREPARING 2-ACETYLTHIO-3-PHENYL-PROPIONIC ACID AND THE SALTS THEREOF
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, (2008/06/13)
It is described a process for preparing 2-acetylthio-3-phenyl-propionic acid and the salts thereof starting from 2-bromo-3-phenyl-propionic acid and potassium thioacetate in an organic solvent and in the presence of a phase transfer catalyst.
Synthesis of optically pure (S)-2-acetylthio-3-benzenepropanoic acid via enzymatic resolution
Zhu, Jingyang,You, Li,Zhao, Shannon X,White, Brenda,Chen, Jason G,Skonezny, Paul M
, p. 7585 - 7587 (2007/10/03)
A method of synthesizing optically pure (S)-2-acetylthio-3-benzenepropanoic acid has been developed and good to excellent enantiomeric excess achieved via enzymatic resolution.
Dynamic resolution of isomers and resolved isomers
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, (2008/06/13)
Provided is a dynamic resolution method of enriching a desired isomer of an alpha-substituted carboxylic acid relative to an undesired isomer, the method comprising: (a) in a solvent, contacting the alpha-substituted carboxylic acid, wherein the alpha sub
Synthesis and Biological Activity of Hydroxamic Acid-Derived Vasopeptidase Inhibitor Analogues
Walz, Andrew J.,Miller, Marvin J.
, p. 2047 - 2050 (2007/10/03)
(Equation Presented) Syntheses of novel hydroxamic acid-derived azepinones containing pendant mercaptoacyl groups or formyl hydroxamates are described. These new analogues of therapeutically important ACE and NEP inhibitors include unprecedented changes a
Process for preparing 2-acetythio-3-phenyl-propionic acid and the salts thereof
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, (2008/06/13)
It is described a process for preparing 2-acetylthio-3-phenyl-propionic acid and the salts thereof starting from 2-bromo-3-phenyl-propionic acid and potassium thioacetate in an organic solvent and in the presence of a phase transfer catalyst.
Synthesis and SAR of thioester and thiol inhibitors of IMP-1 metallo-β-lactamase
Greenlee, Mark L.,Laub, Joanne B.,Balkovec, James M.,Hammond, Milton L.,Hammond, Gail G.,Pompliano, David L.,Epstein-Toney, Jeffrey H.
, p. 2549 - 2554 (2007/10/03)
Potent thioester and thiol inhibitors of IMP-1 metallo-β-lactamase have been synthesized employing a solid-phase Mitsunobu reaction as the key step.
AMINO ACID DERIVATIVE
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, (2008/06/13)
The present invention relates to an amino acid derivative having an angiotensin I-converting enzyme inhibition activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase inhibition activity.This amino acid derivative is represented by the following general formula (I): STR1 wherein R 1 represents a hydrogen atom or an acyl group; R 2 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, an ary group which may have a substituent, a heteroaryl group which may have a substituent, an arylalkyl group which may have a substituent or a heteroarylalkyl group which may have a substituent;m and n represent each independently an integer of 0, 1 or 2 and J represents a cyclic group having an angiotensin I-converting enzyme inhibition activity.
