476445-30-4Relevant articles and documents
MITOTIC KINESIN INHIBITORS
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Page/Page column 49-50, (2008/06/13)
The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
Two-step synthesis of β-alkyl chalcones and their use in the synthesis of 3,5-diaryl-5-alkyl-4,5-dihydropyrazoles
Cox, Christopher D.,Breslin, Michael J.,Mariano, Brenda J.
, p. 1489 - 1493 (2007/10/03)
We report a simple and efficient two-step synthesis of variously substituted β-alkyl chalcones (7) from the corresponding Weinreb amide and a terminal alkyne, and that these chalcones are useful intermediates for the synthesis of medicinally interesting 3,5-diaryl-5-alkyl-4,5-dihydropyrazoles (6). The current methodology allows for the incorporation of many substitution patterns not available from the few previously reported approaches to compounds in this class.
Highly stereoselective addition of stannylcuprates to alkynones
Nielsen, Thomas E.,Cubillo de Dios, Maria A.,Tanner, David
, p. 7309 - 7313 (2007/10/03)
The addition of stannylcuprate reagents such as (Bu3Sn)(PhS)CuLi to alkynones has been found to proceed in high yield and with excellent stereoselectivity for the Z isomer of the product (>95%). The behavior of the stannylcuprates is thus very different from that of their "carbocuprate" counterparts such as Me2CuLi or Me2Cu(CN)Li2 which are nonstereoselective. Furthermore, in contrast to the reactions of (R3Sn)(PhS)CuLi with the corresponding alkynoates, the presence of a proton source in the reaction medium has no effect on the stereoselectivity of the reaction of alkynones.