7677-48-7Relevant academic research and scientific papers
Saccharin Aza Bioisosteres - Synthesis and Preclinical Property Comparisons
Chen, Yantao,Aurell, Carl-Johan,Pettersen, Anna,Lewis, Richard J.,Hayes, Martin A.,Lepist?, Matti,Jonson, Anna C.,Leek, Hanna,Thunberg, Linda
supporting information, p. 672 - 677 (2017/06/13)
Saccharin is a well-known scaffold in drug discovery. Herein, we report the synthesis and preclinical property comparisons of three bioisosteres of saccharin: aza-pseudosaccharins (cluster B), and two new types of aza-saccharins (clusters C and D). We dem
Metal-assisted reactions. Part 29. Structure and hydrogenolysis of C-N bonds in derivatives of aromatic amines. Bond length and electronegativity changes from X-ray crystallographic data
Brigas, Amadeu F.,Clegg, William,Dillon, Christopher J.,Fonseca, Custodia F.C.,Johnstone, Robert A.W.
, p. 1315 - 1324 (2007/10/03)
Pseudosaccharyl and phenyltetrazolyl derivatives 1-6 were prepared with the aim of weakening the originally strong C-N bond in aromatic amines and facilitating its hydrogenolysis. Structural analyses of the amines 1-6 by 1H and 13C NMR spectroscopy and X-ray diffraction methods have revealed major changes in C-N bond lengths on derivatization as a result of changes in conjugation. These changes are discussed in relation to the observed reactivity of compounds 1-6 towards catalytic and non-catalytic C-N bond hydrogenolysis.
Phosphoramides, XIX. Phosphorus Pentoxide Amine Hydrochloride Reagents in the Synthesis of 3-Amino-1,2-benzisothiazole-1,1-dioxides and 3-Aminothienoisothiazole-1,1-dioxides
Jensen, Klaus G.,Pedersen, Erik B.
, p. 1640 - 1643 (2007/10/02)
3-Amino-1,2-benzisothiazole-1,1-dioxides (2b-n) have been prepared by heating saccharin (1) and the hydrochlorides of primary and secondary aliphatic amines with phosphorus pentoxide and N,N-dimethylcyclohexylamine at 240 deg C. 3-Aminothienoisothi
