147959-19-1Relevant articles and documents
Synthesis of sphingosine analogues: Stereoselective synthesis of 3- deoxysphingosine and cis-isomers
Kawate, Tomohiko,Fukuta, Natsuko,Nishida, Atsushi,Nakagawa, Masako
, p. 2116 - 2118 (1997)
Both enantiomers of 3-deoxysphingosine as well as their cis-isomers were synthesized stereoselectively from L- and D-serine.
Bifunctional Tripeptide with a Phosphonic Acid as a Br?nsted Acid for Michael Addition: Mechanistic Insights
Cortes-Clerget, Margery,Jover, Jesús,Dussart, Jade,Kolodziej, Emilie,Monteil, Maelle,Migianu-Griffoni, Evelyne,Gager, Olivier,Deschamp, Julia,Lecouvey, Marc
supporting information, p. 6654 - 6662 (2017/05/15)
Enamine catalysis is a widespread activation mode in the field of organocatalysis and is often encountered in bifunctional organocatalysts. We previously described H-Pro-Pro-pAla-OMe as a bifunctional catalyst for Michael addition between aldehydes and ar
NOVEL QUINOLINE-SUBSTITUTED COMPOUND
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Paragraph 0602-0604, (2016/10/10)
An object to be achieved by the present invention is to provide a novel compound having EGFR inhibitory effects and cell growth inhibitory effects, as well as a medication useful for the prevention and/or treatment of cancer based on the EGFR inhibitory effects. The present invention provides a compound represented by Formula (I) below, or a salt thereof.
Expeditious synthesis of enantiopure, orthogonally protected bis-α-amino acids (OPBAAs) and their use in a study of Nod1 stimulation
Chen, Po-Ting,Lin, Cheng-Kun,Tsai, Chih-Ju,Huang, Duen-Yi,Nien, Fu-Yao,Lin, Wan-Wan,Cheng, Wei-Chieh
, p. 474 - 482 (2015/01/30)
A convenient approach towards the synthesis of orthogonally protected chiral bis-a-amino acids (OPBAAs) is described. The key transformations include: (1) a highly stereoselective conjugation (alkylation) of the Sch?llkopf bislactim ethers and oxazolidinyl alkyl halides to build a backbone skeleton; and (2) our orthogonal protection strategy. A series of enantiopure OPBAAs bearing a variety of alkyl chain as a spacer; two stereogenic centers; and three protecting groups were prepared as examples. These versatile molecules were applied to the synthesis of biologically interesting di- or tri-peptide analogues, including chiral iE-meso-DAP and A-iE-meso-DAP, for the study of Nod1 activation in the innate immune response.
FACTOR XIa INHIBITORS
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Page/Page column 71, (2015/12/09)
The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
Chemo-enzymatic synthesis of the azasugars 1,4-dideoxyallonojirimycin and 1,4-dideoxymannojirimycin
Venkataiah, Mallam,Reddipalli, Gowrisankar,Jasti, Lakshmi Swarnalatha,Fadnavis, Nitin W.
, p. 1855 - 1860 (2012/01/13)
The enzymatic resolution of the N-phenylacetyl derivative of racemic homoserine lactone with penicillin G acylase immobilized on Eupergit C gave (R)-(+)-α-amino-γ-butyrolactone and (S)-(-)-α-N- phenylacetamido-γ-butyrolactone in high enantiomeric purity (ee >99%) and 46-47% yields for each enantiomer. The enantiomers were converted into azasugars 1,4-dideoxyallonojirimycin and 1,4-dideoxymannojirimycin using Wittig olefination, catalytic ring-closing metathesis (RCM), and stereoselective dihydroxylation with OsO4 in 29% overall yield over 11 high yielding steps. Enzyme inhibition studies showed that 1,4-dideoxyallonojirimycin is a better β-glucosidase inhibitor (IC50 32.4 μM toward β-glucosidase from almonds) and a better β-galactosidase inhibitor (IC50 5.9 mM for β-galactosidase from Aspergillus oryzae) than 1,4-dideoxymannojirimycin (IC50 2.86 mM and 12.5 mM for β-glucosidase and β-galactosidase, respectively).
An asymmetric dihydroxylation route to (-)-bulgecinine
Show, Krishanu,Upadhyay, Puspesh K.,Kumar, Pradeep
experimental part, p. 1234 - 1238 (2011/10/19)
The stereoselective synthesis of (-)-bulgecinine is reported from L-aspartic acid using Sharpless asymmetric dihydroxylation and intramolecular cyclization via nucleophilic displacement of a-tosylate as key steps.
PYRROLIDINONE GLUCOKINASE ACTIVATORS
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Page/Page column 73, (2009/10/30)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
Efficient entry to polysubstituted pyrrolizidines, indolizidines and quinolizidines via a sequential reaction process
Ma, Dawei,Zhu, Wei
, p. 1181 - 1184 (2007/10/03)
A sequential SN2-Michael addition-Michael addition reaction process between ω-iodo-α,β-alkynoates and δ- or γ-amino α,β-unsaturated esters is developed, which affords polysubstituted pyrrolizidines, indolizidines or quinolizidines in good yield
IMPROVED PROCEDURE FOR THE PREPARATION OF (4S)- OR (4R)-2,2-DIMETHYL-4-(2-HYDROXETHYL)OXAZOLIDINE-3-CARBOXYLIC ACID ALKYL ESTERS
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Page/Page column 8; 16, (2010/11/23)
The present invention is directed to a process for the preparation of (4S)- or (4R)-2,2-dimethyl-4-(2-hydroxethyl)oxazolidine-3-carboxylic acid alkyl esters. The invention is further directed to an intermediate product from which those alkyl esters may be obtained.