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1
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77953122104
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note
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DAPY is a commonly used abbreviation in the literature for 2,4-dianilinopyrimidines.
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2
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0024239320
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For lead articles on the topic of Privileged Structures, see:
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For lead articles on the topic of Privileged Structures, see:. Evans B.E., Rittle K.E., Bock M.G., DiPardo M.R., Freidinger R.M., Whitter W.L., Lundell G.F., Veber D.F., and Anderson P.S. J. Med. Chem. 31 (1988) 2235-2246
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(1988)
J. Med. Chem.
, vol.31
, pp. 2235-2246
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Evans, B.E.1
Rittle, K.E.2
Bock, M.G.3
DiPardo, M.R.4
Freidinger, R.M.5
Whitter, W.L.6
Lundell, G.F.7
Veber, D.F.8
Anderson, P.S.9
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5
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0842304428
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Bondensgaard K., Ankersen M., Thogersen H., Hansen B.S., Wulff B.S., and Bywater R.P. J. Med. Chem. 47 (2004) 888-899
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(2004)
J. Med. Chem.
, vol.47
, pp. 888-899
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Bondensgaard, K.1
Ankersen, M.2
Thogersen, H.3
Hansen, B.S.4
Wulff, B.S.5
Bywater, R.P.6
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6
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4243159924
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DeSimone R.W., Currie K.S., Mitchell S.A., Darrow J.W., and Pippin D.A. Comb. Chem. High Throughput Screening 7 (2004) 473-493
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(2004)
Comb. Chem. High Throughput Screening
, vol.7
, pp. 473-493
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DeSimone, R.W.1
Currie, K.S.2
Mitchell, S.A.3
Darrow, J.W.4
Pippin, D.A.5
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8
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49449117755
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Harris P.A., Boloor A., Cheung M., Kumar R., Crosby R.M., Davis-Ward R.G., Epperly A.H., Hinkle K.W., Hunter III R.N., Johnson J.H., Knick V.B., Laudeman C.P., Luttrell D.K., Mook R.A., Nolte R.T., Rudolph S.K., Szewczyk J.R., Truesdale A.T., Veal J.M., Wang L., and Stafford J.A. J. Med. Chem. 51 (2008) 4632-4640
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(2008)
J. Med. Chem.
, vol.51
, pp. 4632-4640
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Harris, P.A.1
Boloor, A.2
Cheung, M.3
Kumar, R.4
Crosby, R.M.5
Davis-Ward, R.G.6
Epperly, A.H.7
Hinkle, K.W.8
Hunter III, R.N.9
Johnson, J.H.10
Knick, V.B.11
Laudeman, C.P.12
Luttrell, D.K.13
Mook, R.A.14
Nolte, R.T.15
Rudolph, S.K.16
Szewczyk, J.R.17
Truesdale, A.T.18
Veal, J.M.19
Wang, L.20
Stafford, J.A.21
more..
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11
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17944374798
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Ludovici D.W., De Corte B.L., Kukla M.J.T., Ye H., Ho C.Y., Lichtenstein M.A., Kavash R.W., Andries K., de Béthune M.-P., Azijn H., Pauwels R., Lewi P.J., Heeres J., Loymans L.M.H., de Jonge M.R., Van Aken K.J.A., Daeyaert F.F.D., Das K., Arnold E., and Janssen P.A.J. Bioorg. Med. Chem. Lett. 11 (2001) 2235-2239
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(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2235-2239
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Ludovici, D.W.1
De Corte, B.L.2
Kukla, M.J.T.3
Ye, H.4
Ho, C.Y.5
Lichtenstein, M.A.6
Kavash, R.W.7
Andries, K.8
de Béthune, M.-P.9
Azijn, H.10
Pauwels, R.11
Lewi, P.J.12
Heeres, J.13
Loymans, L.M.H.14
de Jonge, M.R.15
Van Aken, K.J.A.16
Daeyaert, F.F.D.17
Das, K.18
Arnold, E.19
Janssen, P.A.J.20
more..
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12
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20144366006
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Guillemont J., Pasquier E., Palandjian P., Vernier D., Gaurrand S., Lewi P.J., Heeres J., de Jonge M.R., Koymans L.M.H., Daeyaert F.F.D., Vinkers M.H., Arnold E., Das K., Pauwels R., Andries K., de Béthune M.-P., Bettens E., Hertogs K., Wigerinck P., Timmerman P., and Janssen P.A.J. J. Med. Chem. 48 (2005) 2072-2079
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(2005)
J. Med. Chem.
, vol.48
, pp. 2072-2079
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Guillemont, J.1
Pasquier, E.2
Palandjian, P.3
Vernier, D.4
Gaurrand, S.5
Lewi, P.J.6
Heeres, J.7
de Jonge, M.R.8
Koymans, L.M.H.9
Daeyaert, F.F.D.10
Vinkers, M.H.11
Arnold, E.12
Das, K.13
Pauwels, R.14
Andries, K.15
de Béthune, M.-P.16
Bettens, E.17
Hertogs, K.18
Wigerinck, P.19
Timmerman, P.20
Janssen, P.A.J.21
more..
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13
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61749085561
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Pytel D., Sliwinski T., Poplawski T., Ferriola D., and Majsterek I. Anti-Cancer Agents Med. Chem. 9 (2009) 66-76
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(2009)
Anti-Cancer Agents Med. Chem.
, vol.9
, pp. 66-76
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Pytel, D.1
Sliwinski, T.2
Poplawski, T.3
Ferriola, D.4
Majsterek, I.5
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17
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55549143963
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Walker D.P., Bi F.C., Kalgutkar A.S., Bi F.C., Kalgutkar A.S., Bauman J.N., Zhao S.X., Soglia J.R., Aspnes G.E., Kung D.W., Klug-McLeod J., Zawistoski M.P., McGlynn M.A., Oliver R., Dunn M., Li J.-C., Richter D.T., Cooper B.A., Kath J.C., Hulford C.A., Autry C.L., Luzzio M.J., Ung E.J., Roberts W.G., Bonnette P.C., Buckbinder L., Mistry A., Giffor M.C., Han S., and Guzman-Perez A. Bioorg. Med. Chem. Lett. 18 (2008) 6071-6077
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(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 6071-6077
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Walker, D.P.1
Bi, F.C.2
Kalgutkar, A.S.3
Bi, F.C.4
Kalgutkar, A.S.5
Bauman, J.N.6
Zhao, S.X.7
Soglia, J.R.8
Aspnes, G.E.9
Kung, D.W.10
Klug-McLeod, J.11
Zawistoski, M.P.12
McGlynn, M.A.13
Oliver, R.14
Dunn, M.15
Li, J.-C.16
Richter, D.T.17
Cooper, B.A.18
Kath, J.C.19
Hulford, C.A.20
Autry, C.L.21
Luzzio, M.J.22
Ung, E.J.23
Roberts, W.G.24
Bonnette, P.C.25
Buckbinder, L.26
Mistry, A.27
Giffor, M.C.28
Han, S.29
Guzman-Perez, A.30
more..
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77953121068
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Fleming, P. E.; Shi, Z.; Chen, S.; Schmidt, J. F.; Reader, J. C.; Hone, N. D.; Ciavarri, J. P. Preparation of aryl pyrimidines as protein kinase C inhibitors. WO 2005066139. January 10, 2005.
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Fleming, P. E.; Shi, Z.; Chen, S.; Schmidt, J. F.; Reader, J. C.; Hone, N. D.; Ciavarri, J. P. Preparation of aryl pyrimidines as protein kinase C inhibitors. WO 2005066139. January 10, 2005.
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23
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77953123858
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Preparation of pyrrolopyrimidines as protein kinase inhibitors
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WO 2006124863A2, May 15, 2006
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Okram, B.; Ren, P.; Gray, N. Preparation of pyrrolopyrimidines as protein kinase inhibitors. WO 2006124863A2, May 15, 2006.
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Okram, B.1
Ren, P.2
Gray, N.3
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24
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84889379623
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Preparation of substituted pyridines and pyrimidines as vanilloid receptor ligands
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US 2006058308A1, September 13, 2005
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Norman, M. H.; Pettus, L. H.; Wang, X.; Zhu, J. Preparation of substituted pyridines and pyrimidines as vanilloid receptor ligands. US 2006058308A1, September 13, 2005.
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Norman, M.H.1
Pettus, L.H.2
Wang, X.3
Zhu, J.4
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25
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77953123667
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Imidazolo-5-yl-2-anilopyrimidines as agents for the inhibition of cell proliferation
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WO 2006095159A1, March 8, 2005
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Andrews, D.; Finlay, M. R.; Green, C.; Clifford, J.; Oza, V. Imidazolo-5-yl-2-anilopyrimidines as agents for the inhibition of cell proliferation. WO 2006095159A1, March 8, 2005.
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Andrews, D.1
Finlay, M.R.2
Green, C.3
Clifford, J.4
Oza, V.5
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26
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77953119528
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Methods of treating or preventing autoimmune diseases with 2,4-pyrimdinediamine compounds
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WO 2004014382A1, February 19, 2004
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Singh, R.; Argade, A.; Payan, D. G.; Clough, J.; Keim, H.; Sylvain, C.; Li, H.; Bhamidipati, S. Methods of treating or preventing autoimmune diseases with 2,4-pyrimdinediamine compounds. WO 2004014382A1, February 19, 2004.
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Singh, R.1
Argade, A.2
Payan, D.G.3
Clough, J.4
Keim, H.5
Sylvain, C.6
Li, H.7
Bhamidipati, S.8
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27
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12344287922
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Ma H.-R., Wang Y.-Y., Liu P., Li D.-S., Shi Q.-Z., Lee G.-H., and Peng S.-M. Polyhedron 24 (2005) 215-220
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(2005)
Polyhedron
, vol.24
, pp. 215-220
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Ma, H.-R.1
Wang, Y.-Y.2
Liu, P.3
Li, D.-S.4
Shi, Q.-Z.5
Lee, G.-H.6
Peng, S.-M.7
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30
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34948866679
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For examples of 2-heteroarylaminopyrimidines prepared via alternate approaches to direct substitution of heteroarylamines onto 2-chloropyrimidines, see:
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For examples of 2-heteroarylaminopyrimidines prepared via alternate approaches to direct substitution of heteroarylamines onto 2-chloropyrimidines, see:. Schulte II J.P., and Tweedie S.R. Synlett (2007) 2331-2336
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(2007)
Synlett
, pp. 2331-2336
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Schulte II, J.P.1
Tweedie, S.R.2
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31
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8644259161
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Guillaumet G., Garnier E., Audoux J., Pasquinet E., Suzenet F., Poullain D., and Lebret B. J. Org. Chem. 69 (2004) 7809-7815
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(2004)
J. Org. Chem.
, vol.69
, pp. 7809-7815
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Guillaumet, G.1
Garnier, E.2
Audoux, J.3
Pasquinet, E.4
Suzenet, F.5
Poullain, D.6
Lebret, B.7
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32
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77953122352
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Preparation of pyrazolylamino substituted pyrimidines as anticancer agents
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WO Patent 2006117560, November 11
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Scott, D.; Wang, H., Wang, T. Preparation of pyrazolylamino substituted pyrimidines as anticancer agents. WO Patent 2006117560, November 11, 2006.
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(2006)
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Scott, D.1
Wang, H.2
Wang, T.3
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33
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37549015931
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For an interesting discussion of the practical advantages of microwaves, see:
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For an interesting discussion of the practical advantages of microwaves, see:. Kappe C.O., Herrero M.A., and Kremsner J.M. J. Org. Chem. 73 (2008) 36-47
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(2008)
J. Org. Chem.
, vol.73
, pp. 36-47
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Kappe, C.O.1
Herrero, M.A.2
Kremsner, J.M.3
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77953120413
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note
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+ 294.1.
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35
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77953122869
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note
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9e
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38
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77953121773
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note
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NAr conditions; see Ref. 9f.
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39
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77953121049
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note
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Reactions were analyzed by LC-MS and complete conversion was generally observed after 4-6 h.
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40
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77953120250
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note
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The surprising result reported for the formation of 16c (Table 2, entry 2) under microwave conditions is reproducible.
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41
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77953123815
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For information on the status of Dapivirine clinical trials, see: (a) International Partnerships for Microbicides (IPM). http://www.ipm-microbicides.org (accessed October 2009); (b) U.S. National Institutes of Health. http://clinicaltrials.gov (accessed October 2009).
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For information on the status of Dapivirine clinical trials, see: (a) International Partnerships for Microbicides (IPM). http://www.ipm-microbicides.org (accessed October 2009); (b) U.S. National Institutes of Health. http://clinicaltrials.gov (accessed October 2009).
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77953122076
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Freyne, E. J. E, Buijnsters, P. J. J. A, Willems, M, Embrechts, W. C. J, Love, C. J, Janssen, P. A. J, Lewi, P. J, Heeres, J, de Jonge, M. R, Koymans, L. M. H, Vinkers, H. M, Van Aken, K. J. A, Diels, G. S. M. Heteroaryl amines as glycogen sythase kinase 3β inhibitors GSK3 inhibitors, US 7514445 B2, April 7, 2009
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Freyne, E. J. E.; Buijnsters, P. J. J. A.; Willems, M.; Embrechts, W. C. J.; Love, C. J.; Janssen, P. A. J.; Lewi, P. J.; Heeres, J.; de Jonge, M. R.; Koymans, L. M. H.; Vinkers, H. M.; Van Aken, K. J. A.; Diels, G. S. M. Heteroaryl amines as glycogen sythase kinase 3β inhibitors (GSK3 inhibitors). US 7514445 B2, April 7, 2009.
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