Utility of Japp-Klingemann reaction for the preparation of 5-carboxy-6-chloroindole via Fischer indole protocol
5-Carboxy-6-chloroindole, a precursor for p38 kinase inhibitor, was prepared from 4-amino-2-chloro-3-iodobenzoicacid by following the Japp-Klingemann synthetic approach. The structures of the key intermediates were also confirmed by X-ray analyses. Computational analysis was helpful in understanding the importance of the substituents at the cyclization step of the synthesis.
Chen, Yihui,Shibata, Masayuki,Rajeswaran, Manju,Srikrishnan, Thamarapu,Dugar, Sundeep,Pandey, Ravindra K.
p. 2353 - 2356
(2007/10/03)
Indole-type derivatives as inhibitors of p38 kinase
The invention is directed to methods to inhibit p38-α kinase using compounds comprising a phenyl or thienyl coupled through a piperidine or piperazine nucleus to an indole residue wherein the indole residue mandatorily has a substituent on the ring nitrogen which is an amino or substituted amino group.
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Page/Page column 14
(2008/06/13)
Preparation of benzimidazole-5-carboxamides and indole-5-carboxamides to treat cardiac failure and other disorders.
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Page column 28
(2008/06/13)
Oxazoline antiproliferative agents
Compounds having Formula I are useful for treating cancer. Also disclosed are pharmaceutical compositions comprising compounds of Formula I, and methods of treating cancer in a mammal.
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(2008/06/13)
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