Discovery of 3,3′-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction
In studies aimed toward identifying effective and safe inhibitors of kinase signaling cascades that underlie ischemia/reperfusion (I/R) injury, we synthesized a series of pteridines and pyridopyrazines. The design strategy was inspired by the examination
Palanki, Moorthy S. S.,Dneprovskaia, Elena,Doukas, John,Fine, Richard M.,Hood, John,Kang, Xinshan,Lohse, Dan,Martin, Michael,Noronha, Glenn,Soll, Richard M.,Wrasidlo, Wolfgang,Yee, Shiyin,Zhu, Hong
p. 4279 - 4294
(2008/02/13)
A scaleable synthesis of fiduxosin
Fiduxosin (1) has been under development at Abbott Laboratories for the treatment of benign prostatic hyperplasia. A convergent strategy required methodologies for preparation of an enantiomerically pure 3,4-cis-disubstituted pyrrolidine and a 2,3,5-trisubstituted thienopyrazine in a regiospecific manner. A [3+2] cycloaddition of an enantiopure azomethine ylide followed by a diastereoselective crystallization was employed to prepare the benzopyranopyrrolidine in high diastereomeric and enantiomeric purity. Conditions for reduction of an O-aryl lactone susceptible to epimerization were developed, and cyclization of the alcohol/phenol to the ether was accomplished in high yield. The thienopyrazine was prepared by condensation of methyl thioglycolate and a regiospecifically prepared 2-bromo-3-cyano-5-phenylpyrazine. Conditions for effective halogen substitutive deamination to prepare regiospecific trisubstituted pyrazines will be described.
Haight, Anthony R.,Bailey, Anne E.,Baker, William S.,Cain, Michael H.,Copp, Richard R.,Demattei, John A.,Ford, Kelley L.,Henry, Rodger F.,Hsu, Margaret C.,Keyes, Robert F.,King, Steven A.,McLaughlin, Maureen A.,Melcher, Laura M.,Nadler, William R.,Oliver, Patricia A.,Parekh, Shyamal I.,Patel, Hemant H.,Seif, Louis S.,Staeger, Mike A.,Wayne, Gregory S.,Wittenberger, Steven J.,Zhang, Weijiang
supporting information
p. 897 - 902
(2013/09/03)
Reductive decyanation of pyrazinecarbonitriles
Pyrazinecarbonitriles can be decyanated by hydrogenation with platinum on carbon in the presence of activated carbon under acidic conditions. Pyrazine carbonitrile-N-oxides undergo a stepwise reduction to the deoxy-pyrazinecarbonitriles followed by decyan
Albaneze-Walker, Jennifer,Zhao, Matthew,Baker, Melinda D,Dormer, Peter G,McNamara, James
p. 6747 - 6750
(2007/10/03)
Process for preparing 3-alkoxy-5-alkylpyrazin-2-amines
A process for preparing 3-alkoxy-5-alkylpyrazin-2-amines of the general formula: STR1 wherein R1 is a C1-4 -alkyl group or an aryl group and R2 is a C1-4 -alkoxy group or an aryloxy group, starting either from a
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(2008/06/13)
Unequivocal syntheses of 6-methyl- and 6-phenylisoxanthopterin
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Neilsen,Broadbent,Hennen
p. 1621 - 1628
(2007/10/02)
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