130855-30-0Relevant articles and documents
Total synthesis of (±)-paroxetine by diastereoconvergent cobalt-catalysed arylation
Despiau, Carole F.,Dominey, Andrew P.,Harrowven, David C.,Linclau, Bruno
, p. 4335 - 4341 (2014)
A total synthesis of paroxetine is reported, with a diastereoselective and diastereoconvergent cobalt-catalysed sp3-sp2 coupling reaction involving a 3-substituted 4-bromo-N-Boc-piperidine (Boc = tert-butoxycarbonyl) substrate as a key step. A 9:1 diastereoselectivity was obtained, while a control experiment involving a conformationally locked 3-substituted 4-bromo-tert-butyl cyclohexane ring proceeded with essentially complete stereoselectivity.
Stereodivergent α-allylation of linear aldehydes with dual iridium and amine catalysis
Krautwald, Simon,Schafroth, Michael A.,Sarlah, David,Carreira, Erick M.
, p. 3020 - 3023 (2014/03/21)
We describe the fully stereodivergent, dual catalytic α-allylation of linear aldehydes. The reaction proceeds via direct iridium-catalyzed substitution of racemic allylic alcohols with enamines generated in situ. The use of an Ir(P,olefin) complex and a diarylsilyl prolinol ether as catalysts in the presence of dimethylhydrogen phosphate as the promoter proved to be crucial for achieving high enantio- and diastereoselectivity (>99% ee, up to >20:1 dr). The utility of the method is demonstrated in a concise enantioselective synthesis of the antidepressant (-)-paroxetine.
SULFATED GALACTANS WITH ANTITHROMBOTIC ACTIVITY, PHARMACEUTICAL COMPOSITION, METHOD FOR TREATING OR PROPHYLAXIS OF ARTERIAL OR VENOUS THROMBOSIS, METHOD OF EXTRACTION AND USE THEREOF
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Page/Page column 6-7, (2009/12/23)
The present invention relates to low molecular weight sulfated galactans, obtained from algae, particularly genus Botryocladia, preferably species Botryocladia occidentallis, which have no effect on the factor XII activation of the clotting cascade, having antithrombotic heparinoid activity. The present invention also refers to a pharmaceutical composition comprising said sulfated galactans and the use thejreof, as heparin substitute, in the treatment or prophylaxis of arterial or venous thrombosis in humans and animals. Furthermore, the present invention provides a method of extraction of the said sulfated galactans.