20879-18-9Relevant articles and documents
Asymmetric synthesis of β-adrenergic blockers through multistep one-pot transformations involving in situ chiral organocatalyst formation
Wei, Shengwei,Messerer, Regina,Tsogoeva, Svetlana B.
, p. 14380 - 14384 (2011)
Two birds one stone: A new atom-economical one-pot approach to enantioselective chiral drug synthesis, involving in situ multistep organocatalyst formation and the application of the reaction for multistep sequential synthesis of β-adrenergic blockers is disclosed (see scheme).
One-pot route to β-adrenergic blockers via enantioselective organocatalysed epoxidation of terminal alkenes as a key step
Held, Felix E.,Wei, Shengwei,Eder, Kathrin,Tsogoeva, Svetlana B.
, p. 32796 - 32801 (2014/08/18)
A convenient and environmentally attractive one-pot two-step process for the synthesis of β-adrenergic blockers via Shi's organocatalytic epoxidation of terminal alkenes and subsequent aminolysis reaction of epoxides with isopropylamine under mild reaction conditions has been developed. This journal is the Partner Organisations 2014.
Discovery and initial structure-activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists
Barrow, James C,Nantermet, Philippe G,Selnick, Harold G,Glass, Kristen L,Ngo, Phung L,Young, Mary Beth,Pellicore, Janetta M,Breslin, Michael J,Hutchinson, John H,Freidinger, Roger M,Condra, Cindra,Karczewski, Jerzy,Bednar, Rodney A,Gaul, Stanley L,Stern, Andrew,Gould, Robert,Connolly, Thomas M
, p. 2691 - 2696 (2007/10/03)
Thrombin is the most potent agonist of platelet activation, and its effects are predominantly mediated by platelet thrombin receptors. Therefore, antagonists of the thrombin receptor have potential utility for the treatment of thrombotic disorders. Screening of combinatorial libraries revealed 2 to be a potent antagonist of the thrombin receptor. Modifications of this structure produced 11k, which inhibits thrombin receptor stimulated secretion and aggregation of platelets.
A two-step asymmetric synthesis of (R)-monoaryl epoxides using a chiral oxathiane as a recoverable reagent: Application to the preparation of (R)-β-adrenergic compounds
Solladie-Cavallo,Diep-Vohuule
, p. 3494 - 3498 (2007/10/02)
It is shown that chiral oxathiane 1 is a recoverable and efficient chiral auxiliary which provides, in two steps, (R)-monoaryl epoxides in high enantiomeric purity (98% R and 92% R according to the solvent used). (R)-β-Adrenergic compounds (R)-(-)-DCI and