172846-33-2Relevant articles and documents
Phosphinanes and Azaphosphinanes as Potent and Selective Inhibitors of Activated Thrombin-Activatable Fibrinolysis Inhibitor (TAFIa)
Schaffner, Arnaud-Pierre,Sansilvestri-Morel, Patricia,Despaux, Nicole,Ruano, Elisabeth,Persigand, Thierry,Rupin, Alain,Mennecier, Philippe,Vallez, Marie-Odile,Raimbaud, Eric,Desos, Patrice,Gloanec, Philippe
supporting information, p. 3897 - 3910 (2021/05/04)
Selective and potent inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa) have the potential to increase endogenous and therapeutic fibrinolysis and to behave like profibrinolytic agents without the risk of major hemorrhage, since they do not interfere either with platelet activation or with coagulation during blood hemostasis. Therefore, TAFIa inhibitors could be used in at-risk patients for the treatment, prevention, and secondary prevention of stroke, venous thrombosis, and pulmonary embolisms. In this paper, we describe the design, the structure-activity relationship (SAR), and the synthesis of novel, potent, and selective phosphinanes and azaphosphinanes as TAFIa inhibitors. Several highly active azaphosphinanes display attractive properties suitable for further in vivo efficacy studies in thrombosis models.
METHOD FOR PRODUCING POLYALKYLENE GLYCOL DERIVATIVE HAVING AMINO GROUP AT END
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Paragraph 0182-0188, (2016/07/05)
A method simply produces a narrowly distributed and high-purity polyalkylene glycol derivative having an amino group at an end without using a heavy metal catalyst. A method for producing a polyalkylene glycol derivative having an amino group at the end by reacting a compound represented by the general formula (V) with an alkylene oxide, then reacting a reaction product with an electrophile represented by the general formula (I), and deprotecting the obtained product without using a heavy metal: [in-line-formulae]RA3O(RA4O)k-1RA4O?M+??(V)[/in-line-formulae]wherein RA3 represents a linear; branched, or cyclic hydrocarbon group having 1 to 20 carbon atoms; RA4 represents an alkylene group having 2 to 8 carbon atoms; k represents an integer of 2 to 5; and M represents an alkali metal; wherein RA1a and RA1b each independently represent a protective group of the amino group, or one of RA1a and RA1b represents H and the other represents a protective group of the amino group, or RA1a and RA1b bind to each other to form a cyclic protective group, and the protective group is deprotectable without using a heavy metal; RA2 represents a linear, branched, or cyclic hydrocarbon group having 1 to 6 carbon atoms; and X represents a leaving group.
Synthesis of 17H-tetrabenzofluorene derivatives as chiral selectors for enantiomeric separation by HPLC on porous graphitised carbon
Dutton, Jonathan K.,Knox, John H.,Radisson, Xavier,Ritchie, Harold J.,Ramage, Robert
, p. 2581 - 2588 (2007/10/02)
The synthesis of the amides 2 which are designed to be selectors containing the chiral N-(3,5-dinitrobenzoyl)-α-phenylglycine covalently linked to tetrabenzofluorene is described.These amides are strongly adsorbed onto porous graphitised carbon, which affords chiral stationary phases that are able to resolve both racemic aromatic alcohols 3 and the methyl esters of Fmoc amino acids 4 on microgram quantities using high-pressure liquid chromatography.Two methods of preparation of these chiral phases from 2 and porous graphitised carbon are described and the stability of these phases to the chromatographic conditions and to water have also been investigated.