140372-83-4Relevant academic research and scientific papers
Iron-Catalyzed Azidoalkylthiation of Alkenes with Trimethylsilyl Azide and 1-(Alkylthio)pyrrolidine-2,5-diones
Yu, Jipan,Jiang, Min,Song, Zhixuan,He, Tiancheng,Yang, Haijun,Fu, Hua
, p. 2806 - 2810 (2016)
A simple, efficient and practical iron-catalyzed azidoarylthiation of alkenes has been developed at room temperature, and the corresponding products containing ortho-sited sulfide and azide units were obtained in moderate to good yields with good tolerance of functional groups. The protocol uses readily available 1-(alkylthio)pyrrolidine-2,5-diones and trimethylsilyl azide as the alkylthiation and azidation reagents, respectively, inexpensive and environmentally friendly iron chloride as the catalyst without addition of any ligand and additive. (Figure presented.).
Configurational flexibility of epimeric β-aminothioether-chelated ruthenium(II) η6-arene complex salts
Weber, Immo,Heinemann, Frank W.,Bauer, Walter,Zenneck, Ulrich
experimental part, p. 123 - 140 (2009/04/11)
Five chiral β-aminothioethers were obtained via different routes orientated on literature protocols. Three of these β-aminothioethers were reacted with two di-μ-chloro-bis{chloro[η6-arene]- ruthenium(II)} derivatives, resulting in the title complex salts. The complex cations exhibit three stereocenters, viz. ruthenium and sulfur atoms and the chiral benzylic carbon atom of the chelate ligand backbone. Both, ruthenium and sulfur stereocenters epimerize into a mixture of four NMR distinguishable diastereomers in equilibrium, but the designed chiral benzylic carbon atom is stable under all conditions applied so far. The relative diastereomer concentrations in solution depend mainly on the spatial requirements of the η6-arene ligand rather than on the thioether moiety. Diastereomer ratios and the absolute configurations in solution were studied by NMR and CD spectroscopy. The spectroscopic results fit to the absolute X-ray crystal structure parameters determined for the diastereomers present in the crystalline state.
Synthesis of mexiletine analogues from non-activated aziridines
Ingebrigtsen, Truls,Lejon, Tore
, p. 891 - 902 (2008/03/13)
A general method for the synthesis of mexiletine analogues by nucleophilic ring opening of non-activated racemic aziridines has been developed (Scheme 1). Structural variation is introduced by employing different nucleophiles or by altering the substitution on the aziridine ring.
Base-promoted aminoethylation of thiols with 2-oxazolidinones: A simple synthesis of 2-aminoethyl sulfides
Ishibashi, Hiroyuki,Uegaki, Masayuki,Sakai, Manami,Takeda, Yoshifumi
, p. 2115 - 2120 (2007/10/03)
A simple synthesis of 2-aminoethyl sulfides using a base-promoted reaction of 2-oxazolidinones with thiols is described. An application of this method to the synthesis of chiral 2-aminoethyl sulfides and sulfur-containing heterocyclic compounds is also presented.
An efficient procedure for cleavage of aziridines with various thiols promoted by ZnCl2
Wu,Hou,Dai
, p. 1314 - 1317 (2007/10/03)
The ring-opening reaction of aziridines with various thiophenols and thiols catalyzed by ZnCl2 provides β-amino sulfides in high yield.
Anti-tumor compounds
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, (2008/06/13)
The invention relates to quinazoline derivatives, or pharmaceutically-acceptable salts thereof, which possess anti-tumour activity; to processes for their manufacture; and to pharmaceutical compositions containing them. The invention provides a quinazoline of the formula: STR1 wherein R1 includes hydrogen, amino and alkyl or alkoxy each of up to 4 carbon atoms; R2 includes hydrogen, alkyl, hydroxyalkyl and halogenoalkyl each of up to 4 carbon atoms; R3 is hydrogen or alkyl or up to 3 carbon atoms; Ar is phenylene or heterocyclene; L is a group of the formula --CO.NH--, --NH.CO--, --CO.NR4 --, --NR4.CO--, --CH=CH-- or --CO.O--, wherein R4 is alkyl of up to 4 carbon atoms; and Y is a branched alkyl group bearing substituents Y2 and Y3 the definition of each independently including hydroxy, cyano, aryl and heteroaryl, and the definition of Y3 also optionally including sulpho, N-phenylsulphonylcarbamoyl and 5-tetrazolyl; or a pharmaceutically-acceptable salt thereof.
Asymmetric Synthesis of Functionalised Pyrrolidines. Highly Diastereoselective Cyclisations Mediated by Sulfide and Sulfoxide Ligands
Davies, Ian W.,Gallagher, Timothy,Lamont, R. Brian,Scopes, David I.C.
, p. 335 - 337 (2007/10/02)
Silver(I)-catalysed cyclisation of sulfide 1b and sulfoxides 4 and 5 to give the corresponding 2-vinylpyrrolidines 2b, 6a and 7a, respectively proceeds with a high ( up to 99 percent diastereoisomeric excess) level of diastereoselectivity; in all of these
