82199-98-2Relevant academic research and scientific papers
Synthesis of N-protected/free indole-7-carboxaldehyde
Mohanakrishnan, Arasambattu K.,Balamurugan, Ramalingam,Ramesh, Neelamegam,Mathiselvam, Manoharan,Manavalan, Subramaniam
, p. 4343 - 4352 (2008/03/13)
A direct method for the preparation of N-protected/free indole-7-carboxaldehyde is reported from the corresponding N-protected 7-bromomethylindoles using three different conditions. Copyright Taylor & Francis Group, LLC.
Methods and compounds for treating proliferative diseases
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, (2008/06/13)
The compounds disclosed herein are indolocarbazoles of Formula (I), which are potent CDK4 inhibitors, and are useful in the treatment of cell proliferative disorders, including cancer. Formula (I).
PURINE DERIVATIVES AS KINASE INHIBITORS
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Page/Page column 47, (2008/06/13)
The present invention provides kinase inhibitors of Formula I.
KINASE INHIBITORS
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Page/Page column 31, (2010/02/07)
The present invention provides kinase inhibitors of Formula (I)
An improved method for direct conversion of heteroaryl-aldehydes to heteroaryl-acetonitriles
Engler, Thomas A.,Furness, Kelly,Malhotra, Sushant,Diefenbacher, Clive,Clayton, Joshua R.
, p. 2903 - 2905 (2007/10/03)
Treatment of heteroaryl-aldehydes with diethyl cyanophosphonate in the presence of a catalytic amount of LiCN affords phosphorylated cyanohydrins which are reduced in situ with SmI2 to give heteroaryl-acetonitriles in generally good overall yields (50-100%). The generality of the process is demonstrated.
Novel, potent and selective cyclin D1/CDK4 inhibitors: Indolo[6,7-a]pyrrolo[3,4-c]carbazoles
Engler, Thomas A.,Furness, Kelly,Malhotra, Sushant,Sanchez-Martinez, Concha,Shih, Chuan,Xie, Walter,Zhu, Guoxin,Zhou, Xun,Conner, Scott,Faul, Margaret M.,Sullivan, Kevin A.,Kolis, Stanley P.,Brooks, Harold B.,Patel, Bharvin,Schultz, Richard M.,DeHahn, Tammy B.,Kirmani, Kashif,Spencer, Charles D.,Watkins, Scott A.,Considine, Eileen L.,Dempsey, Jack A.,Ogg, Catherine A.,Stamm, Nancy B.,Anderson, Bryan D.,Campbell, Robert M.,Vasudevan, Vasu,Lytle, Michelle L.
, p. 2261 - 2267 (2007/10/03)
The synthesis and CDK inhibitory properties of a series of indolo[6,7-a]pyrrolo[3,4-c]carbazoles is reported. In addition to their potent CDK activity, the compounds display antiproliferative activity against two human cancer cell lines. These inhibitors also effect strong G1 arrest in these cell lines and inhibit Rb phosphorylation at Ser780 consistent with inhibition of cyclin D1/CDK4.
ADDITION OF CARBON NUCLEOPHILES TO ARENE-CHROMIUM COMPLEXES
Semmelhack, M.F.,Clark, G.R.,Garcia, J.L.,Harrison, J.J.,Thebtaranonth, Y.,et. al
, p. 3957 - 3965 (2007/10/02)
The electrophilic reactivity of arenes coordinated to the chromium tricarbonyl unit has been developed into several distinct methods for coupling carbon nucleophiles with aromatic rings.Addition of the nucleophile produces stable η-cyclohexadienyl chromium complexes which can be oxidized to induce loss of the endo hydrogen and the metal, overall nucleophilic substitution for hydrogen.Alternatively, the intermediate can be protonated and the resulting cyclohexa-1,3-diene can be detached from the chromium, effecting nucleophilic addition with reduction of one double bond.If a halogen (F, Cl) is present as a ring substituent, and if the nucleophile can migrate about the arene ligand, then loss of halide can occur parallel with classical nucleophilic aromatic substitution for halogen in electron-deficient haloarenes.With substituted arenes, the regioselectivity of addition becomes important and is often very high.Particularly useful are strong resonance donor substituents (RO-, R2N-, F-) where selectivity for meta attack is high.Indole provides an excellent example of selective activation, as the six-membered ring complexes selectively and is then susceptible to nucleophilic substitution, predominantly at the 4 and 7 positions.Substitution for halogen is a somewhat limited process and depends upon the nature of the nucleophile.Very reactive nucleophiles add to unsubstituted positions and are often slow to isomerize to the ipso position from which loss of halide can occur.
