Total Synthesis of the Claimed Structure of (±)-Hyptinin and Structural Revision of Natural Hyptinin
A total synthesis of (±)-hyptinin was achieved via a convergent route using the key phosphonate, cyclic ketone, and aryl Grignard components. The 1H and 13C NMR spectra of natural hyptinin did not agree with those of the synthesized
Synthesis and biological evaluation of a triazole-based library of pyrido[2,3-d]pyrimidines as FGFR3 tyrosine kinase inhibitors
A library of pyrido[2,3-d]pyrimidines was designed as inhibitors of FGFR3 tyrosine kinase allowing possible interactions with an unexploited region of the ATP binding-site. This library was built-up with an efficient step of click-chemistry giving easy access to triazole-based compounds bearing a large panel of substituents. Among the 27 analogues synthesized, more than half exhibited 55-89% inhibition of in vitro FGFR3 kinase activity at 2 μM and one (19g) was able to inhibit auto-phosphorylation of mutant FGFR3-K650M in transfected HEK cells.
Synthesis of a benzolactone collection using click chemistry
A collection of benzotriazoles consisting of seven compounds was prepared from the propynyl-substituted benzolactone 1 and various azides using click chemistry. The lactone 1 was obtained through a short route by direct esterification of the allylbenzoic
Ritschel, Jan,Sasse, Florenz,Maier, Martin E.
p. 78 - 87
(2007/10/03)
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