Synthesis of RWJ 68354: A potent inhibitor of the MAP kinase p38

Tetrahedron Letters

Volumn 39, Issue 48, 1998, Pages 8763-8764

  Henry, James R ^a   Dodd, John H ^a  

^a R W JOHNSON PHARMACEUTICAL RES I   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

6 AMINO 2 (4 FLUOROPHENYL) 4 METHOXY 3 (4 PYRIDYL) 1H PYRROLO[2,3 B]PYRIDINE; INTERLEUKIN 1; MITOGEN ACTIVATED PROTEIN KINASE; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; SYNAPTOPHYSIN; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG;

ARTICLE; CYTOKINE PRODUCTION; DRUG MECHANISM; DRUG SYNTHESIS; INFLAMMATION; RHEUMATOID ARTHRITIS; SIGNAL TRANSDUCTION;

EID: 0032569867     PISSN: 00404039     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0040-4039(98)01991-1     Document Type: Article

References (8)

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2. 2. Bernstein, J.; Stearns, B.; Shaw, E. Lott, W.A. J. Amer. Chem. Soc. 1947, 69, 1151.
3. 3. Herbert, R., Wibberley, D.G. J. Chem. Soc. (C) 1969, 1505.
4. 4. Senderoff, S.G.; Heys, J.R.; Blackburn, D.W. J. Labelled Compd. Radiopharm. 1987, 24, 971.
5. 5 Gallagher, T.F.; Fier-Thompson, S.M.; Garigipati, R.S.; Sorenson, M.E.; Smietana, J.M.; Lee, D.; Bender, P.E.; Lee, J.C., Laydon, J.T.; Griswold, D.E.; Chabot-Fletcher, M.C.; Breton, J.J.; Adams, J.L. Bioorg. Med. Chem. Lett. 1995, 5, 1171.
6. 6. Markees, D.G.; Dewey, V.C.; Kidder, G.W. J. Med. Chem. 1968, 11, 126.
7. 1H NMR (300 MHz, d6 DMSO) δ 11.5 (s, 1H), 8.4 (d, 2H, J=7.7 Hz), 7.3-7.1 (m, 6H), 5.8 (s, 1H), 5.8 (bs, 2H), 3.7 (s, 3H). MP 279-280 °C.
8. 4 salt of 2. Studies are currently underway to determine the origin of selectivity and mechanism of this reaction.