58402-26-9Relevant academic research and scientific papers
Carboxylation with CO2 via brook rearrangement: Preparation of α-hydroxy acid derivatives
Mita, Tsuyoshi,Higuchi, Yuki,Sato, Yoshihiro
, p. 14 - 17 (2014/01/23)
In the presence of CsF, a wide range of α-substituted α-siloxy silanes were carboxylated under a CO2 atmosphere (1 atm) via Brook rearrangement. A variety of α-substituents including aryl, alkenyl, and alkyl groups were tolerated to afford α-hydroxy acids in moderate-to-high yields. One-pot synthesis from aldehydes using PhMe2SiLi and CO 2 was also possible, providing α-hydroxy acids without the isolation of an α-hydroxy silane.
Discovery of γ-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor α converting enzyme: Design, synthesis, and structure-activity relationships
Duan, James J.-W.,Chen, Lihua,Wasserman, Zelda R.,Lu, Zhonghui,Liu, Rui-Qin,Covington, Maryanne B.,Qian, Mingxin,Hardman, Karl D.,Magolda, Ronald L.,Newton, Robert C.,Christ, David D.,Wexler, Ruth R.,Decicco, Carl P.
, p. 4954 - 4957 (2007/10/03)
New γ-lactam TACE inhibitors were designed from known MMP inhibitors. A homology model of TACE was built and examined to identify the S1′ site as the key area for TACE selectivity over MMPs. Rational exploration of the P1′-S1′ interactions resulted in the discovery of the 3,5-disubstituted benzyl ether as a TACE-selective P1′ group. Further optimization led to the discovery of IK682 as a selective and orally bioavailable TACE inhibitor.
