Tofacitinib demonstrated efficacy vs placebo at Week 16 in Asian patients with moderate to severe plaque psoriasis; efficacy was maintained through Week 52. No unexpected safety findings were observed. [NCT01815424].
Highly enantioselective aldol reactions of aldehydes with cyclic ketones catalyzed by a primary amine derived from cinchonine are reported. Aromatic aldehydes reacted with various cyclic ketones cleanly to afford the anti-aldol adducts in up to 99% yield, with good diastereoselectivities (up to 9 : 1) and excellent enantioselectivities (up to 99% ee).
Palladium-catalyzed asymmetric formal [3 + 2] cycloaddition of vinyl cyclopropanes and aldimines or isatinderived ketimines proceeded smoothly in the presence of chiral phosphoramidite ligands. The corresponding highly functionalized and optically enriched pyrrolidine or spiro-[pyrrolidin-3,2′-oxindole] derivatives are obtained in up to 94% yield and with up to 96% ee and 7:1 dr.
The first copper hydride (CuH)-catalyzed asymmetric 1,6-conjugate reduction of p-quinone methides is reported. This protocol provides a new method to access a variety of triarylmethanes and 1,1,2-triarylethanes in good yields with excellent enantioselectivities and broad functional group tolerance.
Herein,
we report the Pd(0)-catalyzed intermolecular asymmetric
dearomative [3 + 2] annulation of phenols with vinyl cyclopropanes
via in situ generated ortho-quinone methide intermediates.
A series of highly functionalized spiro-[5,6] bicycles which bear
three contiguous stereogenic centers including one all-carbon quaternary
were obtained with excellent stereoselectivities. Density functional
theory (DFT) calculations indicate that the reactions were controlled
by thermodynamics.
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