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(a) Levitzki, A. FASEB 1992, 6, 3276;
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Levitzki, A.1
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(b) For number six in a series on tyrphostins, see: Gazit, A.; Osherov, N.; Gilon, C.; Levitzki, A. J. Med. Chem. 1996, 39, 4905.
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Gazit, A.1
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3
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13344295097
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Meydan, N.; Grunberger, T.; Dadi, H.; Shahar, M.; Arpaia, E.; Lapidot, Z.; Leeder, J. S.; Freedman, M.; Cohen, A.; Gazit, A.; Levitzki, A.; Roifman, C. M. Nature 1996, 379, 645.
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Meydan, N.1
Grunberger, T.2
Dadi, H.3
Shahar, M.4
Arpaia, E.5
Lapidot, Z.6
Leeder, J.S.7
Freedman, M.8
Cohen, A.9
Gazit, A.10
Levitzki, A.11
Roifman, C.M.12
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Kaur, G.; Gazit, A.; Levitzki, A.; Stowe, E.; Cooney, D. A.; Sausville, E. A. Anti-Cancer Drugs 1994, 5(2), 213.
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Levitzki, A.3
Stowe, E.4
Cooney, D.A.5
Sausville, E.A.6
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5
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0345154794
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note
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A "reactor" in the context of "directed sorting" is any discrete item (tube, can, bag, etc.) in or on which a synthesis support (such as polystyrene) can remain physically associated.
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6
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0345586722
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note
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-1 in DMF). Since the time of this study, we have concluded that somewhat lower tube loadings lead to lowered rates of intratube reactivity.
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7
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0345154788
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note
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Tubular reactors prepared as described here, but standardized to ca. 35 μmoles of amine loading/tube, are available commercially: IRORI, La Jolla, CA.
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8
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33748243831
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(a) Nicolaou, K. C.; Xiao, X. Y.; Parandoosh, Z.; Senyei, A.; Nova, M. Angew. Chem. Int. Ed. Engl. 1995, 34, 2289;
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Nicolaou, K.C.1
Xiao, X.Y.2
Parandoosh, Z.3
Senyei, A.4
Nova, M.5
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9
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0028815228
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(b) Moran E. J.; Sarshar S.; Cargill J. F.; Shahbaz M. M.; Lio A.; Mjalli A. M. M.; Armstrong R. W. J. Am. Chem. Soc. 1995, 117, 10787.
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Moran, E.J.1
Sarshar, S.2
Cargill, J.F.3
Shahbaz, M.M.4
Lio, A.5
Mjalli, A.M.M.6
Armstrong, R.W.7
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10
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0345586715
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2. and removal of the Fmoc protecting group with 20% pipendine in DMF at RT.
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11
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0345154775
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Note: In this article, we will utilize a matrix notation to describe sets of reagents serving as diversity inputs [e.g., 6{1-18}], an individual reagent from this set [e.g., 6{6}]. product libraries [e.g., 13{1-18,1-8,1-3}], and an individual product [e.g., 13{ 12.1.3}]. Each diversity-introducing reaction step is represented in order in the matrix descriptor. We also propose (for the sake of brevity) the adjective 'chemset' to refer to a matrix of compounds, to include all the described members of a given compound matrix unless otherwise specified [e.g., chemset 13 is equivalent to 13{1-18,1-8,1-3} within the context of this article, which lists the set of diversity reagents used]. While the traditional use of lowercase letters to describe variants of a compound would avoid the requirement for a new formalism, libraries constructed using diversity steps with more than 26 reagents will always prove cumber-some to depict using letters.
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13
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0000844109
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Abdel-Magid, A. F.; Carson, K. G.; Harris, B. D.; Maryanoff, C. A.; Shah, R. D. J. Org. Chem. 1996, 61, 3849.
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Abdel-Magid, A.F.1
Carson, K.G.2
Harris, B.D.3
Maryanoff, C.A.4
Shah, R.D.5
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14
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0344292413
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Interestingly, we encountered what amounts to a "scale-up" problem in this step inasmuch as the conditions that gave complete chemical conversion using one reactor were insufficient to afford complete conversion when using 432. The difficulty was solved simply by using triple coupling conditions. However, the observation does highlight the fact that reactions for library synthesis must be optimized carefully and the great benefit of monitoring reactions at the library generation stage itself.
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15
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0031151959
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For an overview of encoding benefits and strategies, see: Czarnik, A. W. Curr. Op. Chem. Biol. 1997, 1, 60.
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Curr. Op. Chem. Biol.
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Czarnik, A.W.1
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16
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0344724422
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note
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Of course, it is also straightforward to make a predetermined number of copies of each product if desired.
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17
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0344724279
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The goal of making each library member only once requires that the ID of each reactor be read at the end of each reaction step, so that the subsequent "pooling" step can be accomplished in a nonrandom fashion. For this reason, the use of memory tags that can be both read and written to using rf (which are available) would be an unnecessary functionality.
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18
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0344292406
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note
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It is important to note that one of these "conversions" is, in fact, an identity transformation (i.e., no reaction), so that all compounds 10{a,b,1} are identical to the corresponding compounds 12{a,b,1}.
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19
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0030869479
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Methods for high-throughput NMR are being developed: Keifer, P. A. Drug Discovery Today 1997, 2, 468.
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Drug Discovery Today
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Keifer, P.A.1
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33947092534
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Mitchell, A. R.; Kent, S. B. H.; Engelhard, M.; Merrifield, R. B. J. Org. Chem. 1978, 43, 2845.
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0030792941
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Xiao, X.-Y.; Zhao, C.; Potash, H.; Nova, M. P. Angew. Chem. Int. Ed. Engl. 1997, 36, 780.
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Xiao, X.-Y.1
Zhao, C.2
Potash, H.3
Nova, M.P.4
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