154201-91-9Relevant articles and documents
The alkoxycarbonylation of protected propargyl alcohols
Alam, Md. Mahbubul,Beghetto, V.,Bertoldini, M.,Scrivanti, A.,Sole, R.
, (2020)
Palladium-catalyzed alkoxycarbonylation of the C≡C triple bond of propargyl alcohol is a sustainable synthetic approach to 2-(hydroxymethyl)acrylates, a family of valuable intermediates. The developed synthetic protocol includes protection of the alcoholic function of the alkyne before its carbonylation in the presence of Drent's catalytic system. Protection step effectively extends the catalyst life hence enhancing the practical applicability of the reaction. The effectiveness of some different protecting groups (benzyl, acetyl and trimethylsilyl) has been assessed and the influence of the reaction parameters investigated.
COMPOSITIONS AND METHODS FOR PROTEIN LABELING, MODIFICATION, ANALYSIS, AND TARGETED DELIVERY
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Paragraph 00251, (2020/01/24)
The invention relates to chemically reactive and/or biologically active compounds, reagents and compositions thereof. More particularly, the invention provides novel reagents that are useful in chemical synthesis, functionalization, delivery, probing and/or analytical measurements of small molecule drugs, proteins, antibodies and other biomolecules. The invention provides novel biologically active agents useful as diagnostics or therapeutics, and related composition and methods of uses thereof.
Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: New insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7
Sagot, Emanuelle,Pickering, Darryl S.,Pu, Xiaosui,Umberti, Michelle,Stensb?l, Tine B.,Nielsen, Birgitte,Chapelet, Marion,Bolte, Jean,Gefflaut, Thierry,Bunch, Lennart
experimental part, p. 4093 - 4103 (2009/05/30)
(S)-Glutamic acid (Glu) is the major excitatory neurotransmitter in the central nervous system (CNS) activating the plethora of ionotropic Glu receptors (iGluRs) and metabotropic Glu receptors (mGluRs). In this paper, we present a chemo-enzymatic strategy for the enantioselective synthesis of five new Glu analogues 2a-f (2d is exempt) holding a functionalized substituent in the 4-position. Nine Glu analogues 2a-j are characterized pharmacologically at native 2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA), kainic acid (KA), and N-methyl-D-aspartic acid (NMDA) receptors in rat synaptosomes as well as in binding assays at cloned rat iGluR5-7 subtypes. A detailed in silico study address as to why 2h is a high-affinity ligand at iGluR57 (Ki = 3.81, 123, 57.3 nM, respectively), while 2e is only a high affinity ligand at iGluR5 (Ki = 42.8 nM). Furthermore, a small series of commercially available iGluR ligands are characterized in iGluR5-7 binding.
