210686-42-3Relevant articles and documents
Multistep solid-phase synthesis of an antibiotic and receptor tyrosine kinase inhibitors using the traceless phenylhydrazide linker
Stieber, Frank,Grether, Uwe,Mazitschek, Ralph,Soric, Natascha,Giannis, Athanassios,Waldmann, Herbert
, p. 3282 - 3291 (2003)
The hydrazide group is an oxidatively cleavable traceless linker for solid-phase chemistry. This linker technology was used to develop a multistep solid-phase synthesis of an antibiotic that is active against Mycobacterium tuberculosis. Furthermore, we describe an efficient method for the traceless synthesis of 2-aminothiazoles that display dual inhibitory activity against the receptor tyrosine kinases VEGFR-2 and Tie-2. The synthesis method proceeds through 9 steps on the solid phase and should give access to a much larger library of 2-aminothiazoles, from which a new class of anti-angiogenesis drugs may be developed.
An oxidation-labile traceless linker for solid-phase synthesis
Stieber, Frank,Grether, Uwe,Waldmann, Herbert
, p. 1073 - 1077 (2007/10/03)
Traceless release of biaryls, acetylenes, alkenes, heterocycles, thioethers, and secondary amines from different solid supports can be achieved under very mild conditions by using a hydrazide group. This group, which is converted into an acyl diazene by oxidation and subsequently cleaved by a nucleophile (see scheme), is thus an attractive new linker for solid- phase synthesis and combinatorial chemistry.
