96476-16-3Relevant academic research and scientific papers
An Efficient Ga(OTf)3/Isopropanol Catalytic System for Direct Reduction of Benzylic Alcohols
Sai, Masahiro
supporting information, p. 4330 - 4335 (2018/10/15)
This study aims to report the first gallium-catalyzed direct reduction of benzylic alcohols using isopropanol as a reductant. The reaction proceeds via gallium catalyst-assisted hydride transfer of the in situ-generated benzylic isopropyl ether. The method generates only water and acetone as byproducts and thus provides an atom-economic and environmentally friendly approach to the synthesis of di- and triarylmethanes, which are important substructures in various bioactive compounds and functional materials. (Figure presented.).
Triphenylbutanamines: Kinesin spindle protein inhibitors with in vivo antitumor activity
Wang, Fang,Good, James A. D.,Rath, Oliver,Kaan, Hung Yi Kristal,Sutcliffe, Oliver B.,MacKay, Simon P.,Kozielski, Frank
, p. 1511 - 1525 (2012/04/10)
The human mitotic kinesin Eg5 represents a novel mitotic spindle target for cancer chemotherapy. We previously identified S-trityl-l-cysteine (STLC) and related analogues as selective potent inhibitors of Eg5. We herein report on the development of a series of 4,4,4-triphenylbutan-1-amine inhibitors derived from the STLC scaffold. This new generation systematically improves on potency: the most potent C-trityl analogues exhibit Kiapp ≥ 10 nM and GI50 ≈ 50 nM, comparable to results from the phase II clinical benchmark ispinesib. Crystallographic studies reveal that they adopt the same overall binding configuration as S-trityl analogues at an allosteric site formed by loop L5 of Eg5. Evaluation of their druglike properties reveals favorable profiles for future development and, in the clinical candidate ispinesib, moderate hERG and CYP inhibition. One triphenylbutanamine analogue and ispinesib possess very good bioavailability (51% and 45%, respectively), with the former showing in vivo antitumor growth activity in nude mice xenograft studies.
Sterically Hindered Free Radicals, XIII. Wittig's Radical 4-Benzoyltriphenylmethyl and Analogous Mono-4-substituted Trityl Radicals
Zarkadis, Antonios K.,Neumann, Wilhelm P.,Uzick, Wolfram
, p. 1183 - 1192 (2007/10/02)
The mono-4-R-triphenylmethyl radicals 1, 8b-f, R = tBu, CF3, COMe, COPh, CN, Me, or their quinonoid dimers 4, 9b-f are prepared, most of them for the first time.The degree of dissociation of the latter at 25 deg C is surprisingly high (=/ 33percent, 0.01 M), donors and acceptors being effective here likewise.ESR data are given and discussed.
