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2004
Polyphenyl derivatives
Q 0700
Diaryl-Substituted Salicyl- and Anthranyl-ketoximes as Potential Estrogen
Ligands. — Slight structural modification of two previously reported estro47- 092 Receptor
gen ligands involves the introduction of small alkyl groups on the imine carbon atom.
The syntheses of salicylketoximes (IV) and (X) and anthranyl derivative (XV) are
achieved via intermediates (III), (IX), and (XIV), resp., which are obtained by submitting their corresponding precursors to two identical, sequential Pd-catalyzed cross-coupling steps with phenylboronic acid (II). The synthesis of ketoxime (X) involves a Fries
rearrangement, cf. (VII)→(VIII). The introduction of an alkyl group causes a significant reduction in binding affinity on both receptor subtypes compared to the binding
affinities of the reference compounds. This effect may be due to the loss of planarity of
the pseudocycle, initiated by an interaction between the alkyl group and the spatially
adjacent aromatic hydrogen. — (MINUTOLO, F.; ANTONELLO, M.; BERTINI, S.;
PLACANICA, G.; RAPPOSELLI, S.; CARLSON, K. E.; KATZENELLENBOGEN, J.
A.; MACCHIA*, M.; Farmaco 59 (2004) 8, 601-607; Dip. Sci. Farm., Univ. Pisa,
I-56126 Pisa, Italy; Eng.) — H. Hoennerscheid
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