441014-73-9Relevant articles and documents
2-(1H-INDOLE-3-CARBONYL)-THIAZOLE-4-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ARYL HYDROCARBON RECEPTOR (AHR) AGONISTS FOR THE TREATMENT OF E.G. ANGIOGENESIS IMPLICATED OR INFLAMMATORY DISORDERS
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Paragraph 00162; 00248, (2021/06/26)
2-(1H-lndole-3-carbonyl)-thiazole-4-carboxamide derivatives and the corresponding imidazole, oxazole and thiophene derivatives and related compounds as aryl hydrocarbon receptor (AHR) agonists for the treatment of angiogenesis implicated disorders, such as e.g. retinopathy, psoriasis, rheumatoid arthritis, obesity and cancer, or inflammatory disorders. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 27 to 32 and 59 to 219; examples 1 to 8; compounds 1-1 to 1-97; tables 1-a, 2 and 3).
Mild and selective silicon-mediated access to enantioenriched 1,2-mercaptoamines and β-amino arylchalcogenides
Tanini, Damiano,Borgogni, Cosimo,Capperucci, Antonella
supporting information, p. 6388 - 6393 (2019/04/25)
Metal-free ring opening reactions of activated and unactivated aziridines with different silyl chalcogenides are described. Judicious tuning of the reaction conditions enables the synthesis of chiral enantioenriched N-Ts and N-Boc 1,2-mercaptoamines in good yields from the corresponding aziridines and bis(trimethylsilyl)sulfide. N-Protected and N-H unactivated aziridines are efficiently converted into the corresponding β-arylchalcogeno amines upon treatment with suitable arylchalcogenosilanes. The silicon-mediated ring opening reactions proceed with excellent regioselectivity and stereospecificity, allowing to access a wide array of synthetically and biologically valuable enantioenriched chalcogenoamines.
Aziridines ring opening by silyl chalcogenides: A stereoselective access to polyfunctionalized molecules as precursor of sulfurated and selenated heterocycles
Tanini, Damiano,Barchielli, Giulia,Benelli, Francesca,Deglinnocenti, Alessandro,Capperucci, Antonella
, p. 1265 - 1270 (2015/08/18)
Aziridines react efficiently with bis(trimethyl)silyl-sulfide and -selenide to afford a direct access to β-amino thiols and selenols. Synthesis of 2,4-disubstituted 1,3-selenazolidines is obtained through reaction of 1,2-amino selenols with aldehydes.
Simple preparation of N-protected chiral-amino alkyl thiols from corresponding iodides employing sodium trithiocarbonate
Madhu, Chilakapati,Hemantha, H. P.,Vishwanatha, T. M.,Sureshbabu, V. V.
, p. 228 - 235,8 (2020/09/02)
A simple protocol for the preparation of N-protected amino alkyl thiols is reported that employs a reaction of sodium trithiocarbonate (Na 2CS3) with N-protected amino alkyl iodides. Na 2CS3 is easy to prepare and the protocol circumvents the use of strong bases and multiple steps. All the thiol compounds made were obtained as enantiopure samples and were characterized employing NMR and mass spectrometry.
Computer-assisted discovery of novel amino acid derived sulfides for enantioselective epoxidation of aldehydes
Myllym?ki, Vesa T.,Lindvall, Mika K.,Koskinen, Ari M. P.
, p. 4629 - 4635 (2007/10/03)
With the aid of molecular modeling, thiazolidine derivatives have been designed as catalysts for epoxidation of aldehydes. Accessible from amino acids, the thiazolidine derivatives can be synthesized in both enantiomeric forms and with a diverse array of substituents. A representative member, (S)-N-tert-butoxycarbonyl-2,2-dimethyl-4-isopropyl thiazolidine, of the thiazolidine family has been prepared, and it has been shown to catalyze the formation of trans-stilbene oxide with high enantioselectivity. Experimental and theoretical characterization has allowed the evaluation of the factors affecting enantioselectivity, facilitating the design of second-generation thiazolidines and other chiral sulfides as epoxidation catalysts.
