52485-06-0Relevant articles and documents
Bisindolyl maleimide derivative and preparation method and application thereof
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Paragraph 0797, (2017/01/02)
The invention provides a bisindolyl maleimide derivative and a preparation method and application thereof. The bisindolyl maleimide derivative has an excellent alpha-glucosidase inhibition effect and can be used for preventing and treating diabetes.
Bisindolylmaleimide derivative, and preparation method and use thereof
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Paragraph 0800, (2017/04/03)
The invention provides a bisindolylmaleimide derivative, and a preparation method and a use thereof. The bisindolylmaleimide derivative has a good tumor treatment effect, especially has a good treatment effect on some drug-resistant tumors, and can realize accurate treatment of the drug-resistant tumors.
NaBH3CN: A janus substitute for tin-free radical-based reactions
Guiard, Julie,Rahali, Yaniss,Praly, Jean-Pierre
supporting information, p. 4461 - 4466 (2014/08/05)
Beside showing that thermal radical reactions (reduction, Giese reaction) are efficient if bromo-/iodosugars are treated with NaBH3CN and 2,2″-azobisisobutyronitrile, we explored new initiation conditions on the basis of CuI salts (≤0.5 equiv.) supposed to produce radicals from organobromides through a set. This was confirmed, as at about 50 C under an inert atmosphere acetobromoglucose was reduced to the rearranged 2-deoxyglucose and as N-allyl α-bromoamides reacted, depending on the conditions, either by reductive cyclization or atom-transfer radical cyclization. A related cyclization occurred upon using Cu(OAc)2. This and other assays showed the reduction by NaBH3CN of CuII salts, either added or formed in situ. Having both ionic and radical reactivity, NaBH 3CN appears as a Janus reagent that may be useful for tin-free radical chemistry under mild and very simple conditions. Copyright
Rapid access to in situ generated (R)- and (S)-2-furyloxirane and associated regioselective nucleophilic ring-opening studies
Porzelle, Achim,Gordon, Victoria A.,Williams, Craig M.
, p. 1619 - 1621 (2008/02/05)
Reported herein is the facile preparation of (R)- and (S)-2-furyloxirane from D- and L-tri-O-acetyl glucal and associated regioselective nucleophilic ring-opening studies. Georg Thieme Verlag Stuttgart.
Syntheses of l-glucosamine donors for 1,2-trans-glycosylation reactions
Lafont, Dominique,Boullanger, Paul
, p. 3368 - 3379 (2007/10/03)
Two new l-glucosamine donors, that is pent-4-enyl 3,4,6-tri-O-acetyl-2-allyloxycarbonylamino-2-deoxy-β-l-glucopyranos ide 16 and ethyl 3,4,6-tri-O-acetyl-2-allyloxycarbonylamino-2-deoxy-1-thio-β-l-gluco pyranoside 21 were prepared in 12 steps from l-arabinose. The reaction pathway uses 3,4,6-tri-O-acetyl-l-glucal 5, and then 3,4,6-tri-O-acetyl-2-deoxy-2-iodo-α-l-mannopyranosyl azide 8 as intermediates. The latter, together with donors 16 and 21, were used for preparing l-glucosamine neoglycolipids.
A systematic investigation of the synthetic utility of glycopeptide glycosyltransferases
Oberthuer, Markus,Leimkuhler, Catherine,Kruger, Ryan G.,Lu, Wei,Walsh, Christopher T.,Kahne, Daniel
, p. 10747 - 10752 (2007/10/03)
Glycosyltransferases involved in the biosynthesis of bacterial secondary metabolites may be useful for the generation of sugar-modified analogues of bioactive natural products. Some glycosyltransferases have relaxed substrate specificity, and it has been assumed that promiscuity is a feature of the class. As part of a program to explore the synthetic utility of these enzymes, we have analyzed the substrate selectivity of glycosyltransferases that attach similar 2-deoxy-L-sugars to glycopeptide aglycons of the vancomycin-type, using purified enzymes and chemically synthesized TDP β-2-deoxy-L-sugar analogues. We show that while some of these glycopeptide glycosyltransferases are promiscuous, others tolerate only minor modifications in the substrates they will handle. For example, the glycosyltransferases GtfC and GtfD, which transfer 4-epi-L-vancosamine and L-vancosamine to C-2 of the glucose unit of vancomycin pseudoaglycon and chloroorienticin B, respectively, show moderately relaxed donor substrate specificities for the glycosylation of their natural aglycons. In contrast, GtfA, a transferase attaching 4-epi-L-vancosamine to a benzylic position, only utilizes donors that are closely related to its natural TDP sugar substrate. Our data also show that the spectrum of donors utilized by a given enzyme can depend on whether the natural acceptor or an analogue is used, and that GtfD is the most versatile enzyme for the synthesis of vancomycin analogues.
An easy approach for the acetylation of saccharidic alcohols. Applicability for regioselective protections
Adinolfi, Matteo,Barone, Gaspare,Iadonisi, Alfonso,Schiattarella, Marialuisa
, p. 4661 - 4663 (2007/10/03)
Cheap 4 ? molecular sieves can promote acetylation of carbohydrate hydroxyl functions with Ac2O in absence of any co-reagent. The procedure is compatible with the presence of a variety of acid labile protecting groups and can be exploited for regioselective protections.