119-54-0Relevant academic research and scientific papers
Insertion of arynes into N-halo bonds: A direct approach to O -haloaminoarenes
Hendrick, Charles E.,McDonald, Stacey L.,Wang, Qiu
, p. 3444 - 3447 (2013/07/26)
A new approach to access o-haloaminoarenes has been achieved by insertion of arynes into a nitrogen-halide bond (N-X). This transition-metal-free transformation displays a broad substrate scope of arynes, good compatibility with functional groups, and high regioselectivity. Representative transformations of the o-haloaminoarenes are described to highlight their utility for rapid access to diversely functionalized aminoarene derivatives.
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors
Sutton, James C.,Bolton, Scott A.,Hartl, Karen S.,Huang, Ming-Hsing,Jacobs, Glenn,Meng, Wei,Ogletree, Martin L.,Pi, Zulan,Schumacher, William A.,Seiler, Steven M.,Slusarchyk, William A.,Treuner, Uwe,Zahler, Robert,Zhao, Guohua,Bisacchi, Gregory S.
, p. 3229 - 3233 (2007/10/03)
A series of N1-activated C4-carboxy azetidinones was prepared and tested as inhibitors of human tryptase. The key stereochemical and functional features required for potency, serine protease specificity and aqueous stability were determined. From these studies compound 2, BMS-262084, was identified as a potent and selective tryptase inhibitor which, when dosed intratracheally in ovalbumin-sensitized guinea pigs, reduced allergen-induced bronchoconstriction and inflammatory cell infiltration into the lung.
Studies in Potential Filaricides: Part XV - Synthesis of 1-Acyl/Aryl-4-substituted-piperazines as Diethylcarbamazine Analogs
Agrawal, V. K.,Sharma, Satyavan
, p. 650 - 654 (2007/10/02)
1-Acyl-4-substituted-piperazines (4-29) have been prepared starting from 1-benzylpiperazine while 1-aryl-4-aroylpiperazines (30-44) have been obtained from the corresponding 1-arylpiperazines.None of the compounds shows any significant filaricidal activity against Litomosoides carinii in cotton rats and cestodicial activity against Hymenolepis nana in mice.
