-
4
-
-
0032542115
-
-
and references cited therein
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d) S. Booth, P. H. H. Hermkens, H. C. J. Ottenheijm, D. C. Rees; Tetrahedron, 1998, 54, 15385-15443 and references cited therein;
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Tetrahedron
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-
Booth, S.1
Hermkens, P.H.H.2
Ottenheijm, H.C.J.3
Rees, D.C.4
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5
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-
0000144719
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-
e) F. Balkenhohl, C. Von den Busshe-Hünnefeld, A. Lansky, C. Zechel, Angew. Chem. 1996, 108, 2436-2487; Angew. Chem. Int. Ed. Engl. 1996, 35, 2288-2337;
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-
Balkenhohl, F.1
Von Den Busshe-Hünnefeld, C.2
Lansky, A.3
Zechel, C.4
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6
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0030477258
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e) F. Balkenhohl, C. Von den Busshe-Hünnefeld, A. Lansky, C. Zechel, Angew. Chem. 1996, 108, 2436-2487; Angew. Chem. Int. Ed. Engl. 1996, 35, 2288-2337;
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8
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0028243847
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g) E. M. Gordon, R. W. Barrett, W. J. Dower, S. P. A. Fodor, M. A. Gallop, J. Med. Chem. 1994, 37, 1233-1251;
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J. Med. Chem.
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Gordon, E.M.1
Barrett, R.W.2
Dower, W.J.3
Fodor, S.P.A.4
Gallop, M.A.5
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9
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0028318863
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h) E. M. Gordon, R. W. Barrett, W. J. Dower, S. P. A. Fodor, M. A. Gallop, J. Med. Chem. 1994, 37, 1385-1401.
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Gordon, E.M.1
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Dower, W.J.3
Fodor, S.P.A.4
Gallop, M.A.5
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10
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0032925557
-
-
For reviews on M-CRs see: a) S. L. Dax, J. J. McNally, M. A. Youngman, Curr. Med. Chem. 1999, 6, 255-270;
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Dax, S.L.1
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12
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0000512227
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c) R. W. Armstrong, A. P. Combs, P. A. Tempest, S. D. Brown, T. A. Keating, Acc. Chem. Res. 1996, 29, 123-131;
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Armstrong, R.W.1
Combs, A.P.2
Tempest, P.A.3
Brown, S.D.4
Keating, T.A.5
-
14
-
-
85037477925
-
-
The histogram featured on Figure 2 is based on data collected from the Chemical Abstract Database with the help of the interrogation program CAPLUS. It summarized the publications in which appear, either in the abstract and/or the title, either of the keywords multicomponent, three-component, four-component, multi[]component, three[]component, four[]component and []reaction
-
The histogram featured on Figure 2 is based on data collected from the Chemical Abstract Database with the help of the interrogation program CAPLUS. It summarized the publications in which appear, either in the abstract and/or the title, either of the keywords multicomponent, three-component, four-component, multi[]component, three[]component, four[]component and []reaction.
-
-
-
-
15
-
-
85037465570
-
-
The recent rise of interest for M-CRs, is best exemplified by the first international conference on the topic (M-CR 2000) to take place in München (Germany) in October 2000
-
The recent rise of interest for M-CRs, is best exemplified by the first international conference on the topic (M-CR 2000) to take place in München (Germany) in October 2000.
-
-
-
-
16
-
-
0025893762
-
-
The solid-phase "split-mix" protocol for instance, which is an elegant way of creating large collections of related molecules has been extensively reviewed elsewhere and will not be considered further here. See, for example: a) A. Furka, F. Sebestyén, M. Asgedom, G. Dibo, Int. J. Pept. Res. 1991, 37, 487-493;
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Int. J. Pept. Res.
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-
-
Furka, A.1
Sebestyén, F.2
Asgedom, M.3
Dibo, G.4
-
17
-
-
0026419328
-
-
as well as references given in ref. [1]
-
b) K. S. Lam, S. E. Salmon, E. M. Hersh, V. J. Hruby, W. M. Kazmierski, R. J. Knapp, Nature, 1991, 354, 82-84; as well as references given in ref. [1].
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(1991)
Nature
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, pp. 82-84
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-
Lam, K.S.1
Salmon, S.E.2
Hersh, E.M.3
Hruby, V.J.4
Kazmierski, W.M.5
Knapp, R.J.6
-
18
-
-
85037468074
-
-
note
-
[17] let us only consider complexity as a function of molecular weight, number and order of chemical bonds, stereocenters, heteroatoms, cycles, and overall symmetry among other parameters. In the present context of drug design, a successful drug candidate will achieve a task of predefined refinement, notably by interacting simultaneously with several complementary functions in a receptor binding pocket or by exhibiting a combination of properties and reactivities, which correlates with the presence of several structural features in a well-defined spatial arrangement. One might therefore anticipate that elaborated tasks need a sufficient level of drug complexity to be successfully achieved. As the demand on drug efficacy will continue to expand in the years to come, there is little doubt that structural complexity of future drugs will follow (genetargeted antisens drugs certainly pave the way in that direction).
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-
-
-
19
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0001166252
-
-
For descriptions of molecular complexity see: a) H. W. Whitlock, J. Org. Chem. 1998, 63, 7982-7989;
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J. Org. Chem.
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Whitlock, H.W.1
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22
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0000846320
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C. H. Heatchcock, Angew. Chem. 1992, 104, 675-691; Angew. Chem. Int. Ed. Engl. 1992, 31, 665-681.
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Angew. Chem.
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Heatchcock, C.H.1
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23
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33748232292
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C. H. Heatchcock, Angew. Chem. 1992, 104, 675-691; Angew. Chem. Int. Ed. Engl. 1992, 31, 665-681.
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Angew. Chem. Int. Ed. Engl.
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-
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26
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0000791854
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c) B. M. Trost, Angew. Chem. 1995, 107, 285-307; Angew. Chem. Int. Ed. Engl. 1995, 34, 259-281;
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Trost, B.M.1
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27
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33750309194
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c) B. M. Trost, Angew. Chem. 1995, 107, 285-307; Angew. Chem. Int. Ed. Engl. 1995, 34, 259-281;
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28
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0026418434
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d) B. M. Trost, Science 1991, 254, 1471-1477.
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Science
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Trost, B.M.1
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29
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0343239973
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a) L. Velluz, J. Valls, J. Mathieu; Angew. Chem. 1967,79, 774-785; Angew. Chem. Int. Ed. Engl. 1967, 6,778-789;
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Velluz, L.1
Valls, J.2
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30
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84981825269
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a) L. Velluz, J. Valls, J. Mathieu; Angew. Chem. 1967,79, 774-785; Angew. Chem. Int. Ed. Engl. 1967, 6,778-789;
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32
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0012714486
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Including "target family-directed libraries", see: C. J. Burns, R. D. Groneberg, J. M. Salvino, G. McGeehan, S. M. Condon, R. Morris, M. Morisette, R. Mathew, S. Darnbrough, K. Neuenschwander, A. Scotese, S. W. Djuric, J. Ullrich, R. Labaudiniere, Angew. Chem. 1998, 110, 3044-3047; Angew. Chem. Int. Ed. 1998, 37, 2848-2550, and references cited therein.
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Burns, C.J.1
Groneberg, R.D.2
Salvino, J.M.3
McGeehan, G.4
Condon, S.M.5
Morris, R.6
Morisette, M.7
Mathew, R.8
Darnbrough, S.9
Neuenschwander, K.10
Scotese, A.11
Djuric, S.W.12
Ullrich, J.13
Labaudiniere, R.14
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33
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0032476829
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and references cited therein
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Including "target family-directed libraries", see: C. J. Burns, R. D. Groneberg, J. M. Salvino, G. McGeehan, S. M. Condon, R. Morris, M. Morisette, R. Mathew, S. Darnbrough, K. Neuenschwander, A. Scotese, S. W. Djuric, J. Ullrich, R. Labaudiniere, Angew. Chem. 1998, 110, 3044-3047; Angew. Chem. Int. Ed. 1998, 37, 2848-2550, and references cited therein.
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a) I. Ugi, A. Dömling, W. Hörl, Endeavour 1994, 18, 115-122;
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Ugi, I.1
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0001505321
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c) I. Ugi, M. Goebel, B. Gruber, M. Heilingbrunner, C. Heiß, W. Hörl, O. Kern, M. Starneker, Res. Chem. Intermed. 1996, 22, 625-644.
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Hörl, W.6
Kern, O.7
Starneker, M.8
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42
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0032563923
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Aminodiacetic adducts
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Aminodiacetic adducts: a) S. J. Park, G. Keum, S. B. Kang, H. Y. Koh, Y. Kim, D. H. Lee, Tetrahedron Lett. 1998, 39, 7109-7112;
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Park, S.J.1
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Lee, D.H.6
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0001560402
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b) I. Ugi, W. Hörl, C. Hanush-Kompa, T. Schmid, E. Herdtweck, Heterocycles 1998, 47, 965-975;
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Ugi, I.1
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44
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c) B. M. Ebert, I. K. Ugi, M. Grosche, E. Herdtweck, W. A. Herrmann, Tetrahedron, 1998, 54, 11887-11898;
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Ebert, B.M.1
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0001238690
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d) A. Demharter, W. Hörl, E. Herdtweck, I. Ugi, Angew. Chem. 1996, 108, 185-187; Angew. Chem. Int. Ed. Engl. 1996, 35, 173-175;
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Demharter, A.1
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46
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0347915136
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d) A. Demharter, W. Hörl, E. Herdtweck, I. Ugi, Angew. Chem. 1996, 108, 185-187; Angew. Chem. Int. Ed. Engl. 1996, 35, 173-175;
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47
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e) I. Ugi, A. Demharter, W. Hörl, T. Schmid, Tetrahedron 1996, 52, 11657-11664;
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Tetrahedron
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Ugi, I.1
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48
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0001505096
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lactams: f) I. Ugi, Angew. Chem. 1982, 94, 826-835; Angew. Chem. Int. Ed. Engl. 1982, 21, 810-819;
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Ugi, I.1
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49
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0020211577
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lactams: f) I. Ugi, Angew. Chem. 1982, 94, 826-835; Angew. Chem. Int. Ed. Engl. 1982, 21, 810-819;
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Angew. Chem. Int. Ed. Engl.
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50
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g) A. Failli, H. Immer, M. Götz, Can. J. Chem. 1979, 57, 3257-3261.
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51
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0033546342
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T. Lindhorst, H. Bock, I. Ugi, Tetrahedron Lett. 1999, 55, 7411-7420; besides cyclohexenylisocyanide other options have been proposed, see: A. M. M. Mjalli, S. Sepehr, T. J. Baiga, Tetrahedron Lett. 1996, 37, 2943-2946.
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Tetrahedron Lett.
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Lindhorst, T.1
Bock, H.2
Ugi, I.3
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52
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0029940759
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T. Lindhorst, H. Bock, I. Ugi, Tetrahedron Lett. 1999, 55, 7411-7420; besides cyclohexenylisocyanide other options have been proposed, see: A. M. M. Mjalli, S. Sepehr, T. J. Baiga, Tetrahedron Lett. 1996, 37, 2943-2946.
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Tetrahedron Lett.
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Mjalli, A.M.M.1
Sepehr, S.2
Baiga, T.J.3
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53
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a) C. Hulme, J. Peng, S-Y. Tang, C. J. Burns, I. Morize, R. Labaudinière, J. Org. Chem. 1998, 63, 8021-8023;
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Hulme, C.1
Peng, J.2
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Morize, I.5
Labaudinière, R.6
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55
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a) C. Hulme, J. Peng, B. Louridas, P. Menard, P. Krolikowski, N. Vasant Kumar, Tetrahedron Lett. 1998, 39, 8047-8050;
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Hulme, C.1
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Menard, P.4
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b) C. Hulme, M. Morissette, F. Volz, C. J. Burns, Tetrahedron Lett. 1998, 39, 1113-1116.
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Hulme, C.1
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57
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85037462069
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unpublished results
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C. Hulme, unpublished results.
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Hulme, C.1
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0030063277
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b) A. M. Strocker, T. A. Keating, P. A. Tempest, R. W. Armstrong, Tetrahedron Lett. 1996, 37, 1149-1152;
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Strocker, A.M.1
Keating, T.A.2
Tempest, P.A.3
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0029940759
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c) A. M. M. Mjalli, S. Sarshar, T. J. Baiga, Tetrahedron Lett. 1996, 37, 2943-2946.
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0031661388
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a) H. Bienaymé, K. Bouzid, Angew. Chem. 1998, 110, 2349-2352; Angew. Chem. Int. Ed. 1998, 37, 2234-2237;
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66
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0032575201
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d) C. Blackburn, B. Guan, P. Fleming, K. Shiosaki, S. Tsai, Tetrahedron Lett. 1998, 39, 3635-3638.
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Blackburn, C.1
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0031549105
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a) M. A. Marx, A.-L. Grillot, C. T. Lower, K. A. Breaver, P. A. Bartlett, J. Am. Chem. Soc. 1997, 119, 6153-6167;
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Marx, M.A.1
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68
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0029944026
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b) B. C. Hamper, D. R. Dukesherer, M. S. South, Tetrahedron Lett. 1997, 37, 3671-3674;
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Hamper, B.C.1
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0029042575
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c) M. M. Murphy, J. R. Schullek, E. M. Gordon, M. A. Gallop, J. Am. Chem. Soc. 1995, 117, 7029-7030;
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Murphy, M.M.1
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Gallop, M.A.4
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72
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0032537090
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D. Fokas, W. J. Ryan, D. S. Casebier, D. L. Coffen, Tetrahedron Lett. 1998, 39, 2235-2238.
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Fokas, D.1
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73
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0032537015
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a) R. Baudelle, P. Melnyk, B. Déprez, A. Tartar, Tetrahedron, 1998, 54, 4125-4140;
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Tetrahedron
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Baudelle, R.1
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75
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0030829336
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c) R. Annunziata, M. Cinquini, F. Cozzi, V. Molteni, O. Schupp, Tetrahedron 1997, 53, 9715-9726;
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M. Cavicchioli, E. Sixdenier, A. Derrey, D. Bouyssi, G. Balme, Tetrahedron Lett. 1997, 38, 1763-1766.
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79
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0030801516
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For another interesting example see: R. Grigg, S. Brown, V. Sriharan, M. D. Uttley, Tetrahedron Lett. 1997, 38, 5031-5034.
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For a high throughput purification methods review, see: R. Ferritto, P. Seneci, Drugs Future 1998, 23, 643-654.
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D. P. Sutherlin, T. M. Stark, R. Hughes, R. W. Armstrong, J. Org. Chem. 1996, 61, 8350-8354.
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85033819544
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The first and most famous cascade of two three-component reactions is already eighty years old: The Robinson tropinone synthesis
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