159028-45-2Relevant academic research and scientific papers
Palladium- and Rhodium-Catalyzed Dynamic Kinetic Resolution of Racemic Internal Allenes Towards Chiral Pyrazoles
Hilpert, Lukas J.,Sieger, Simon V.,Haydl, Alexander M.,Breit, Bernhard
supporting information, p. 3378 - 3381 (2019/02/06)
A complementing Pd- and Rh-catalyzed dynamic kinetic resolution (DKR) of racemic allenes leading to N-allylated pyrazoles is described. Such compounds are of enormous interest in medicinal chemistry as certified drugs and potential drug candidates. The new methods feature high chemo-, regio- and enantioselectivities aside from displaying a broad substrate scope and functional group compatibility. A mechanistic rational accounting for allene racemization and trans-alkene selectivity is discussed.
Facile Alder-Ene Reactions of Silylallenes Involving an Allenic C(sp2)-H Bond
Sabbasani, Venkata R.,Huang, Genping,Xia, Yuanzhi,Lee, Daesung
, p. 17210 - 17214 (2016/01/25)
Facile and selective Alder-ene reactions of silylallenes involving the activation of an allenic C(sp2)-H over an allylic C(sp3)-H bond is described. In this ene reaction, the presence of a silyl substituent was found to be critical for the observed reactivity and selectivity since the corresponding alkyl-substituted allenes show different reaction profiles. Computational studies show that the origin of this unusual reactivity is the lower bond dissociation energy of the α-C(sp2)-H bond in silylallenes compared to the corresponding nonsilylated allenes.
Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: Identification of new scaffolds for potent EGFR tyrosine kinase inhibitors
Kitano, Yasunori,Suzuki, Tsuyoshi,Kawahara, Eiji,Yamazaki, Takahisa
, p. 5863 - 5867 (2008/04/03)
The present study identified several 4-alkynyl and 4-alkenylquinazolines that serve as novel and potent EGFR tyrosine kinase inhibitors. The IC50 values of these compounds are in the nanomolar range. In addition, the 4-(4-phenylbut-1-yn/en-yl)q
PtCl2- and PtCl4-catalyzed cycloisomerization of polyunsaturated precursors
Marco-Contelles, Jose,Arroyo, Nieves,Anjum, Shazia,Mainetti, Emily,Marion, Nicolas,Cariou, Kevin,Lemiere, Gilles,Mouries, Virginie,Fensterbank, Louis,Malacria, Max
, p. 4618 - 4633 (2007/10/03)
The PtCl2- and PtCl4-catalyzed cycloisomerization of polyunsaturated precursors with different O-protecting groups at the propargylic position is reported. The free hydroxy, O-(bromomethyl)dimethylsilyl, O-methyl and O-propenyl deriv
The Resolution of Tertiary α-Acetylene- Acetate Esters by the Lipase from Candida Cylindracea
O'Hagan, David,Zaidi, Naveed A.
, p. 1111 - 1118 (2007/10/02)
The resolution of tertiary alcohols using the Candida cylindracea lipase is explored.In particular strategies are deployed to limit nonenzymatic hydrolysis of the tertiary acetate substrates in buffer, such that a full range of the steric requirements and
