- Saccharin Aza Bioisosteres - Synthesis and Preclinical Property Comparisons
-
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
- 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)
-
- 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
-
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
- Jensen, Klaus G.,Pedersen, Erik B.
-
p. 1640 - 1643
(2007/10/02)
-
- 3-Substituted benzisothiazole, 1,1-dioxides
-
3-Substituted benzisothiazole, 1,1-dioxides are provided having the structure STR1 wherein R is hydrogen, halogen, lower alkyl, lower alkoxy, or nitro; R1 is hydrogen, lower alkoxy or halogen with the proviso that R1 can be lower alk
- -
-
-