- One-electron Oxidation of 2,2-dimethyl-2-silaindane by Potassium 12-Tungstocobaltate(III). Lack of Evidence for Stereoelectronic Effects on the Cleavage of a β-Carbon-Silicon Bond in an Aromatic Cation Radical
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The one electron transfer oxidation of 2,2-dimethyl-2-silaindane by K5CoIIIW12O40 leads, in a slow step, to a radical cation which then undergoes fast C-Si bond cleavage, thus indicating that the rate of this cleavage is not significantly affected by the orientation of the C-Si bond with respect to the aromatic system.
- Baciocchi, Enrico,Bernini, Roberta,Lanzalunga, Osvaldo
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- Modular Synthesis of Diverse Natural Product-Like Macrocycles: Discovery of Hits with Antimycobacterial Activity
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A modular synthetic approach was developed in which variation of the triplets of building blocks used enabled systematic variation of the macrocyclic scaffolds prepared. The approach was demonstrated in the synthesis of 17 diverse natural product-like macrocyclic scaffolds of varied (12–20-membered) ring size. The biological relevance of the chemical space explored was demonstrated through the discovery of a series of macrocycles with significant antimycobacterial activity.
- Dow, Mark,Marchetti, Francesco,Abrahams, Katherine A.,Vaz, Luis,Besra, Gurdyal S.,Warriner, Stuart,Nelson, Adam
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p. 7207 - 7211
(2017/05/31)
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- Enantio- and diastereoselective synthesis of highly substituted benzazepines by a multicomponent strategy coupled with organocatalytic and enzymatic procedures
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Enantiomerically pure 4,5-dihydro-1H-benzo[c]azepines with three contiguous stereogenic centers have been assembled by convergent strategy with a good control of diastereoselectivity. The two steps are as follows: an asymmetric organocatalytic Mannich reaction performed on Boc-imines of o-(azidomethyl) benzaldehydes, followed by a one-pot Staudinger/aza-Wittig/Ugi-Joullie sequence. The latter reaction represents one of the first examples of diastereoselective Ugi three-component reaction on a seven-membered cyclic imine. The o-azidomethylbenzaldehydes have been synthesized employing a simple and efficient chemoenzymatic strategy from commercially available building blocks.
- Moni, Lisa,Banfi, Luca,Basso, Andrea,Galatini, Andrea,Spallarossa, Martina,Riva, Renata
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p. 339 - 351
(2014/01/17)
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- Synthesis of novel isochromene derivatives by tandem Ugi reaction/ nucleophilic substitution
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Unprecedented 3-amino-4-amido-lH-isochromenes have been prepared in three steps from protected ortho-(hydroxymethyl)benzaldehyde, with the introduction of three diversity inputs, through a Ugi reaction followed by intramolecular nucleophilic substitution. Georg Thieme Verlag Stuttgart.
- Banfi, Luca,Basso, Andrea,Casuscelli, Francesco,Guanti, Giuseppe,Naz, Farah,Riva, Renata,Zito, Paola
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p. 85 - 88
(2010/07/16)
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- Imidazopyridine compounds and processes for preparation thereof
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The invention relates to an imidazopyridine compound of the formula: STR1 wherein R1 is lower alkynyl, lower alkynyloxy(lower)alkyl or N,N-di(lower)alkylamino(lower)alkynyl, R2 is lower alkyl, R3 is mono (or di or tri)-phenyl(lower)alkyl substituted by one or more substituent(s) selected from cyano, carbamoyl, mono (or di or tri(phenyl(lower)alkylamino, acylamino, carboxy, esterified carboxy, hydroxy, hydroxy(lower)alkyl, acyloxy(lower)alkyl, acyloxy, mono (or di or tri)phenyl(lower)alkoxy, lower alkoxy(lower)alkoxy, tetrahydropyranyloxy, and acylamino(lower)alkyl or mono (or di or tri) phenyl(lower)alkyl substituted by lower alkyl and one additional substituent selected from hydroxy(lower)alkyl, amino, N-lower alkyl-N-acylamino, mono (or di or tri)phenyl(lower)alkylamino, acylamino and lower alkylamino, and R4 is hydrogen or lower alkyl, and a pharmaceutically acceptable salt thereof, useful in the treatment of ulcers.
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