96308-48-4Relevant articles and documents
Design, synthesis, and discovery of a novel CCR1 antagonist
Naya,Sagara,Ohwaki,Saeki,Ichikawa,Iwasawa,Noguchi,Ohtake
, p. 1429 - 1435 (2001)
The CC chemokines may play an important role in the pathogenesis of chronic inflammatory diseases including rheumatoid arthritis, and their effects are thought to be mediated through CCR1 receptors. Several nonpeptide CCR1 receptor antagonists that showed
Enantioselective aziridination of cyclic enals facilitated by the fluorine-iminium ion Gauche effect
Molnar, Istvan Gabor,Tanzer, Eva-Maria,Daniliuc, Constantin,Gilmour, Ryan
supporting information, p. 794 - 800 (2014/01/23)
The enantioselective, organocatalytic aziridination of small, medium and macro-cyclic enals is reported using (S)-2-(fluorodiphenyl methyl)-pyrrolidine. Central to the reaction design is the reversible formation of a β-fluoroiminium ion intermediate, which is pre-organised on account of the fluorine-iminium ion gauche effect. This conformational effect positions the fluorine substituent synclinal-endo to the electropositive nitrogen centre thus benefiting from favourable stereoelectronic and electrostatic interactions (σC-H→σC-F*; F δ-···N+). Consequently, one of the shielding groups on the fluorine-bearing carbon atom is positioned above the π-system, forming the basis of an enantioinduction strategy. Treatment of this intermediate with a "nitrene" source furnished a series of novel, optically active aziridines (e.r. up to 99.5:0.5). Further derivatisation of the product aziridines gives facile access to various amino acid derivatives, including β-fluoroamino acids. Crystallographic analyses of both the aziridines and their derivatives are disclosed. Copyright
Cyclic compounds and uses thereof
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, (2008/06/13)
Compounds of general formula (1) R1—X1—W—X2—Z1—Z2—R2 or salts thereof, exhibiting preventive and therapeutic effects against HIV infectious diseases wherein R1is an optionally substituted five- or six-membered ring group; X1is a free valency or the like; W is a divalent group represented by, e. g., general formula (2) (wherein A and B are each an optionally substituted five- to seven-membered ring; E1and E4are each optionally substituted carbon or the like; E2and E3are each oxygen or the like; and a and b are each a single bond or a double bond); X2is a divalent group constituting a straight chain moiety; Z1is a divalent cyclic group or the like; Z2is a free valency or the like; and R2is optionally substituted amino or the like.
