Site-selective mono-oxidative addition of active zinc into carbon-bromine bond of dibrominated-thiophenes: Preparation of thienylzinc reagents and their applications
A facile protocol for the preparation of 3-bromo-2-thienylzinc bromide A and 5-bromo-2-thienylzinc bromide B has been developed. It has been successfully accomplished by a site-selective oxidative addition of active zinc into a chemically pseudo-equivalent or equivalent carbon-bromine bond, respectively. The subsequent cross-coupling reactions of the organozincs were also successfully carried out under mild conditions providing the corresponding products in moderate to high yields.
Jung, Hye-Soo,Cho, Hyun-Hee,Kim, Seung-Hoi
p. 960 - 964
(2013/02/25)
Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L
A series of thiosemicarbazone analogs based on the benzophenone, thiophene, pyridine, and fluorene molecular frameworks has been prepared by chemical synthesis and evaluated as small-molecule inhibitors of the cysteine proteases cathepsin L and cathepsin B. The two most potent inhibitors of cathepsin L in this series (IC50 50 = 150.8 nM). Bromine substitution in the thiophene series results in compounds that demonstrate only moderate inhibition of cathepsin L. The two most active analogs in the benzophenone thiosemicarbazone series are highly selective for their inhibition of cathepsin L versus cathepsin B.
Kumar, G.D. Kishore,Chavarria, Gustavo E.,Charlton-Sevcik, Amanda K.,Yoo, Grace Kim,Song, Jiangli,Strecker, Tracy E.,Siim, Bronwyn G.,Chaplin, David J.,Trawick, Mary Lynn,Pinney, Kevin G.
supporting information; experimental part
p. 6610 - 6615
(2010/12/20)
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