6265-30-1Relevant articles and documents
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Harvey
, p. 1121 (1949)
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Pyrrolidine synthesis on polystyrene supports: Development of a 'one-pot' dipolar cycloaddition strategy
Barrett, Anthony G.M.,Boffey, Raymond J.,Frederiksen, Mathias U.,Newton, Christopher G.,Roberts, Richard S.
, p. 5579 - 5581 (2001)
Preparation of substituted pyrrolidines was achieved by solid-phase synthesis via a room temperature 1,3-dipolar cycloaddition of a silver-azomethine ylide, generated in situ, with a polymer-supported maleimide.
PROCESS FOR THE INDUSTRIAL SYNTHESIS OF LURASIDONE
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Page/Page column 13, (2015/05/05)
Disclosed is a process for the industrial synthesis of Lurasidone from (1R,2R)-cyclohexane-1,2-diyldimethanol (1), 3-(piperazin-1- yl)benzo[d]isothiazole (3) and (3aR,4R,7R,7aS)-3a,4,7,7a-tetrahydro-4,7- methanoisobenzofuran-1,3-dione (6).). Said process is optimised to obtain Lurasidone with high yields and high purities by preparing highly pure synthesis intermediates, using critical raw materials and reagents in amounts close to the stoichiometric amounts, increasing productivity and reducing the costs and environmental impact of the process.
IBX-mediated oxidation of unactivated cyclic amines: application in highly diastereoselective oxidative Ugi-type and aza-Friedel-Crafts reactions
De Graaff,Bensch,Van Lint, Matthijs J.,Ruijter,Orru
supporting information, p. 10108 - 10112 (2015/10/20)
The first o-iodoxybenzoic acid (IBX) mediated oxidation of unactivated amines to imines is described. A range of meso-pyrrolidines were shown to be suitable substrates. The chemical space was further explored with one-pot oxidative Ugi-type and aza-Friedel-Crafts reactions, which proved to be highly diastereoselective.