123168-37-6Relevant articles and documents
CHEMICAL COMPOUNDS
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Page/Page column 137, (2010/07/10)
The invention is directed to 6-(4-pyι?midinyl)-1 H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R1 - R4 are defined herein. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
A simple stereoselective synthesis of enantiopure 2-substituted pyrrolidines and piperidines from chiral (R)-phenylglycinol-derived bicyclic 1,3-oxazolidines
Andres, Jose M.,Herraiz-Sierra, Ignacio,Pedrosa, Rafael,Perez-Encabo, Alfonso
, p. 1719 - 1726 (2007/10/03)
Chiral, nonracemic 2-substituted pyrrolidines and piperidines were prepared in high ee and moderate to good chemical yields in three steps from (R)-phenylglycinol and γ- or δ-chloroketones. The key step of the synthesis was the stereo- selective reductive ring-opening of chiral bicyclic 1,3- oxazolidines prepared by condensation of (R)-phenylglycinol and the corresponding ketones.
Direct Asymmetric Synthesis of Quaternary Carbon Centers via Addition-Elimination Process: Nitroolefination of α-Substituted δ-Lactones
Fuji, Kaoru,Node, Manabu,Nagasawa, Hideko,Naniwa, Yoshimitsu,Taga, Tooru,et al.
, p. 7921 - 7925 (2007/10/02)
The reactions of chiral nitro enamines 2a-c with zinc enolates 4-6 of α-substituted δ-lactones afforded α,α-disubstituted δ-lactones with a high ee through an addition-elimination process.The best results were obtained with the reaction of 2c with 5.Michael-type addition of the enolate onto the nitro enamine is kinetically controlled and decides the absolute stereochemistry of the product.A cyclic transition model is proposed to rationalize the S-selectivity.