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5
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33746547860
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For an excellent leading reference, see
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For an excellent leading reference, see. Yang L., Zhou C., Guo L., Morriello G., Butora G., Pasternak A., Parsons W.H., Mills S.G., MacCoss M., Vicario P.P., Zweerink H., Ayala J.M., Goyal S., Hanlon W.A., Cascieri M.A., and Springer M.S. Bioorg. Med. Chem. Lett. 14 (2006) 3735
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Zweerink, H.11
Ayala, J.M.12
Goyal, S.13
Hanlon, W.A.14
Cascieri, M.A.15
Springer, M.S.16
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6
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34548589723
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Shiota, T.; Kataoka, K.; Imai, M.; Tsutsumi, T.; Sudoh, M.; Sogawa, R.; Morita, T.; Hada, T.; Muroga, Y.; Takenouchi, O.; Furuya, M.; Endo, N.; Tarby, C. M.; Moree, W.; Teig, S. WO PCT 99/25686.
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7
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5344256233
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Moree W., Kataoka K., Ramirez-Weinhouse M.M., Shiota T., Imai M., Sudo M., Tsutsumi T., Endo N., Muroga Y., Hada T., Tanaka H., Morita T., Greene J., Barnum D., Saunders J., Kato Y., Myers P.L., and Tarby C.M. Bioorg. Med. Chem. Lett. 14 (2004) 5413
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8
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34548552073
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note
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For details on the biological assays and chemical synthesis, see: Carter, P. H.; Cherney, R. J. WO/PCT 2002050019.
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9
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34548594711
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note
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An automated peptide synthesizer was used to load the protected diaminoacid onto resin and to perform steps j and k.
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10
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34548584514
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note
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Compounds 3a and 3b were synthesized by performing steps e and f before steps c and d (Scheme 1).
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-
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12
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34548589722
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3P/DEAD, or DBU/DPPA failed.
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14
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0029866699
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β-Elimination of serine can be surpressed using N-trityl protection See In our hand, use of N-Trityl Thr led to aziridine formation
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β-Elimination of serine can be surpressed using N-trityl protection See. Cherney R.J. J. Org. Chem. 61 (1996) 2544 In our hand, use of N-Trityl Thr led to aziridine formation
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Cherney, R.J.1
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15
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34548596096
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note
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Modification of the carboxamide used acid 2b. Modification of the benzyl amine followed Scheme 1. Modification of the benzamide entailed introducing the benzylamine first (steps e, f), followed by reprotecting with CbzCl, Boc deprotection and amide formation (steps c and d), and hydrogenolysis.
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16
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0037009275
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Duffy J.L., Kevin N.J., Kirk B.A., Chapman K.T., Schleif W.A., Olsen D.B., Stahlhut M., Rutkowski C.A., Kuo L.C., Jin L., Lin J.H., Emini E.A., and Tata J.R. Bioorg. Med. Chem. Lett. 12 (2002) 2423
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Kuo, L.C.9
Jin, L.10
Lin, J.H.11
Emini, E.A.12
Tata, J.R.13
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17
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34548545860
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Cherney, R. J.; Mo, R.; Meyer, D. T.; Nelson, D. J.; Lo, Y. C.; Yang, G.; Scherle, P. A.; Mandlekar, S.; Wasserman, Z.; Jezak, H.; Solomon, K. A.; Tebben, A. J.; Carter, P. H.; Decicco, C. P. Abstracts of Papers, 233 rd ACS National Meeting, Chicago, IL, 2007, MEDI-241.
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20144365483
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De Lucca G.V., Kim U.T., Vargo B.J., Duncia J.V., Santella III J.B., Gardner D.S., Zheng C., Liauw A., Wang Z., Emmett G., Wacker D.A., Welch P.K., Covington M., Stowell N.C., Wadman E.A., Das A.M., Davies P., Yeleswaram S., Graden D.M., Solomon K.A., Newton R.C., Trainor G.L., Decicco C.P., and Ko S.S. J. Med. Chem. 48 (2005) 2194
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Santella III, J.B.5
Gardner, D.S.6
Zheng, C.7
Liauw, A.8
Wang, Z.9
Emmett, G.10
Wacker, D.A.11
Welch, P.K.12
Covington, M.13
Stowell, N.C.14
Wadman, E.A.15
Das, A.M.16
Davies, P.17
Yeleswaram, S.18
Graden, D.M.19
Solomon, K.A.20
Newton, R.C.21
Trainor, G.L.22
Decicco, C.P.23
Ko, S.S.24
more..
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20
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0141678849
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Berkhout T.A., Blaney F.E., Bridges A.M., Cooper D.G., Forbes I.T., Gribble A.D., Groot P.H.E., Hardy A., Ife R.J., Kaur R., Moores K.E., Shillito H., Willetts J., and Witherington J. J. Med. Chem. 46 (2003) 4070
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Berkhout, T.A.1
Blaney, F.E.2
Bridges, A.M.3
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Forbes, I.T.5
Gribble, A.D.6
Groot, P.H.E.7
Hardy, A.8
Ife, R.J.9
Kaur, R.10
Moores, K.E.11
Shillito, H.12
Willetts, J.13
Witherington, J.14
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21
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34548571394
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Dinchuk, J. E.; Davies, P.; Zhao, Q.; Carter, P. H.; Solomon, K. A.; Scherle, P. A. PCT WO 2005049799.
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