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A general structure-activity relationship was defined by Brickner: S. J. Brickner, D. K. Hutchinson, M. R. Barbachyn, P. R. Manninen, D. A. Ulanowicz, S. A. Garmon, K. C. Grega, S. K. Hendges, D. S. Toops, C. W. Ford, G. E. Zurenko, J. Med. Chem. 1996, 39, 673-679.
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[4b] A first outline of our methodology was published in a previous communication: P. ten Holte, L. Thijs, B. Zwanenburg, Tetrahedron Lett. 1998, 39, 7407-7410.
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0004288927
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PS-TsCl, 1.34 mmol/g. Purchased from Argonaut Technologies Inc.
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PS-TsCl, 1.34 mmol/g. Purchased from Argonaut Technologies Inc.
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7
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N2-type cyclization/cleavages are known: [7a] T. Takahashi, S. Tomida, H. Inoue, T. Doi, Synlett 1998, 1261-1263. -
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0004322852
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note
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The average overall yield of 70% reported in the previous communication (ref. 4b) was obtained in a multi-gram scale experiment with Dowex 50X2-400 ion-exchange resin-derived sulfonyl chloride.
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14
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25 = -150.0 ± 0.9 (c = 0.93, acetonitrile).
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21
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0004228118
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note
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13C NMR of sample 5f did not reveal any impurities; nevertheless no reliable elemental analysis of compound 5f could be obtained.
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