75646-21-8Relevant academic research and scientific papers
Synthesis and evaluation of tetrahydroisoquinoline derivatives against Trypanosoma brucei rhodesiense
Cullen, Danica R.,Gallagher, Ashlee,Duncan, Caitlin L.,Pengon, Jutharat,Rattanajak, Roonglawan,Chaplin, Jason,Gunosewoyo, Hendra,Kamchonwongpaisan, Sumalee,Payne, Alan,Mocerino, Mauro
, (2021/10/07)
Human African Trypanosomiasis (HAT) is a neglected tropical disease caused by the parasitic protozoan Trypanosoma brucei (T. b.), and affects communities in sub-Saharan Africa. Previously, analogues of a tetrahydroisoquinoline scaffold were reported as having in vitro activity (IC50 = 0.25–70.5 μM) against T. b. rhodesiense. In this study the synthesis and antitrypanosomal activity of 80 compounds based around a core tetrahydroisoquinoline scaffold are reported. A detailed structure activity relationship was revealed, and five derivatives (two of which have been previously reported) with inhibition of T. b. rhodesiense growth in the sub-micromolar range were identified. Four of these (3c, 12b, 17b and 26a) were also found to have good selectivity over mammalian cells (SI > 50). Calculated logD values and preliminary ADME studies predict that these compounds are likely to have good absorption and metabolic stability, with the ability to passively permeate the blood brain barrier. This makes them excellent leads for a blood-brain barrier permeable antitrypanosomal scaffold.
Iron(II)-Catalyzed Site-Selective Functionalization of Unactivated C(sp3)?H Bonds Guided by Alkoxyl Radicals
Guan, Honghao,Sun, Shutao,Mao, Ying,Chen, Lei,Lu, Ran,Huang, Jiancheng,Liu, Lei
supporting information, p. 11413 - 11417 (2018/08/28)
An alkoxyl radical guided strategy for site-selective functionalization of unactivated methylene and methine C?H bonds enabled by an FeII-catalyzed redox process is described. The mild, expeditious, and modular protocol allows efficient remote aliphatic fluorination, chlorination, amination, and alkynylation of structurally and electronically varied primary, secondary, and tertiary hydroperoxides with excellent functional-group tolerance. The application for one-pot 1,4-hydroxyl functionalization of non-oxygenated alkane substrates initiated by aerobic C?H oxygenation is also demonstrated.
Preparation and palladium-mediated cross-coupling of α- benzoyloxyalkylzinc bromides
Sakata, Komei,Urabe, Daisuke,Inoue, Masayuki
supporting information, p. 4189 - 4192 (2013/07/26)
Here we report a two-step preparation protocol of α- benzoyloxyalkylzinc bromides from α-benzoyloxyalkyl selenides, and their application to palladium-catalyzed cross-coupling reactions with aryl and vinyl iodides. The developed method effectively provides a variety of benzoyl-protected benzylic and allylic alcohol derivatives through the formation of C(sp3)-C(sp2) bonds without affecting various polar functional groups.
DERIVATlVES OF UREA AND RELATED DIAMINES, METHODS FOR THEIR MANUFACTURE AND USES THEREFOR
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Page/Page column 71, (2009/03/07)
The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes
