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Facile, fmoc-compatible solid-phase synthesis of peptide C-terminal thioesters.
A short route to peptide C-terminal thioesters was developed that does not require the use of special linkers or resins and is compatible with standard Fmoc chemistry. Following conventionalExpand
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Polymer-supported Mukaiyama reagent: a useful coupling reagent for the synthesis of esters and amides.
Polymer-supported N-alkyl-2-chloro pyridinium triflate was synthesized in one step from Wang resin. This reagent proved to be a very effective coupling reagent for the synthesis of esters or amidesExpand
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Discovery of a novel series of potent S1P1 agonists.
The discovery of a novel series of S1P1 agonists is described. Starting from a micromolar HTS positive, iterative optimization gave rise to several single-digit nanomolar S1P1 agonists. The compoundsExpand
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Synthesis of 2,2-dimethyl-4-cyclopentene-1,3-dione and 5,5-dimethyl-4-hydroxy-2-cyclopenten-1-one
Abstract Enedione 1 and related rac- and optically active enones 2 bearing a hydroxyl- 2a or a protected- 2b-c or an activated- 2d 4-hydroxyl group at C-4 have been efficiently synthesized from cheapExpand
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Copper-catalyzed three-component synthesis of 5-acetamidoimidazoles from carbodiimides, acyl chlorides and isocyanides
Only very limited methods are available for the synthesis of 5-amino imidazoles. We report in this paper that three-component reaction of acyl chlorides, carbodiimides and α-isocyanoacetates orExpand
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A straightforward, one-pot protocol for the preparation of libraries of 2-oxazolines.
A practical protocol for the parallel synthesis of 2-oxazolines using polymer-supported reagents is described. Polymer-supported Mukaiyama reagent is used to couple a carboxylic acid with an aminoExpand
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A straightforward, one-pot protocol for the synthesis of fused 3-aminotriazoles.
A simple protocol for the synthesis of 3-amino-[1,2,4]triazolo[4,3-a]pyridines is reported. The newly developed one-pot methodology involves the reaction of hydrazinopyridine with isothiocyanates toExpand
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Novel synthesis of vinyl cyclopropane carboxylic acids: Application to the synthesis of (d,l)- and (d)-cis-chrysanthemic acid
Abstract Reaction of sulfur ylides with suitably 4-functionalized-5,5-dimethyl-2-cyclopentenones allows an efficient entry to the bicyclo[3.1.0]hexan-2-one skeleton which proved to be a valuableExpand
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