106403-99-0Relevant academic research and scientific papers
Synthesis of α-methylstilbenes using an aqueous Wittig methodology and application toward the development of potent human aromatase inhibitors
Nielsen, Alexander J.,Raez-Villanueva, Sergio,Crankshaw, Denis J.,Holloway, Alison C.,McNulty, James
supporting information, p. 1395 - 1398 (2019/04/03)
The development of aqueous Wittig methodology for the synthesis of α-methylstilbenes using tripropylphosphine-derived phosphonium salts is described. The Wittig olefination reaction was high yielding and allowed isolation of stilbenes by simple filtration and washing with water. The novel phosphonium salts employed were accessed via a highly efficient, regioselective addition of hydrogen bromide to styrenes. Application of the α-methylstilbenes toward the synthesis of a collection of stilbenoid-triazoles is reported and their inhibition of CYP450 19A1 (aromatase) investigated. The overall structure-activity profile provided additional evidence on the aryl halide-ketone bioisostere hypothesis and identified 6c as a potent inhibitor of aromatase in vitro (Ki = 8 nM).
Heterocyclic chemistry
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, (2008/06/13)
The present invention relates to therapeutically active azaheterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake.
One Pot Synthesis of p-Polyphenyls via the Intramolecular Cyclization of 3-Dimethylaminohex-5-en-1-ynes
Unroe, Marilyn R.,Reinhardt, Bruce A.
, p. 981 - 986 (2007/10/02)
Para linked polyphenyls of various molecular weights are conveniently synthesized from p-bis(3-dimethylamino-1-propynyl)arenes and 1-aryl-2-propenyl bromides in moderate yields using a three step, one-pot procedure.
