147269-61-2Relevant articles and documents
Synthesis of an optically active, bicyclic 2-pyridone dipeptide mimetic
Dragovich, Peter S.,Zhou, Ru,Prins, Thomas J.
, p. 741 - 746 (2007/10/03)
The eleven-step preparation of the bicyclic 2-pyridone dipeptide mimetic 1 [(3S)-6-(benzyloxycarbonylamino)-5-oxo-l,2,3,5-tetrahydroindolizine-3- carboxylic acid] in optically active form (60% ee) is described. Key steps in the synthesis of I include the osmium-catalyzed asymmetric dihydroxylation of olefin 13 [(6-but-3-enyl-2-methoxypyridin-3-yl)carbamic acid benzyl ester] and the intramolecular cyclization of protected diol 19 [(3'R)-{6-[4'-(tert-butyldimethylsilanyloxy)-3'-hydroxybutyl]-2- methoxypyridin-3-yl}carbamic acid benzyl ester] to afford the pyridinium salt 20 [(3S)-[3-(tert-butyldimethylsilanyloxymethyl)-5-methoxy-2,3-dihydro-1H- indolizin-6-yl]carbamic acid benzyl ester trifuoromethanesulfonic acid salt]. Several alternate methods to prepare olefin 13 are also discussed.
Aromatic heterocyclic derivatives as enzyme inhibitors
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Page column 51, (2010/02/04)
The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
ANTITHROMBOTIC AGENTS
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, (2008/06/13)
Compounds of formula (I): Are antithrombotic agents, having utility in a variety of therapeutic areas including the prevention and/or treatment of deep vein thrombosis (DVT) after surgery, major medical illness, paralysis, malignancy, prolonged immobilisa
