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1
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4243965641
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1. (a) The thematic combinatorial issue of Chemical Reviews: Chem. Rev. 1997, 97(2);
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(b) Section 1 in Annual Reports in Combinatorial Chemsitry and Molecular Diversity Vol. 1, ESCOM Pub., 1997, Ed. W.H. Moos, M.R. Pavia, B.K. Kay, A.D. Ellington;
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Annual Reports in Combinatorial Chemsitry and Molecular Diversity Vol. 1
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Moos, W.H.1
Pavia, M.R.2
Kay, B.K.3
Ellington, A.D.4
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3
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0029930278
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(c) Hermkens, P.H.H.; Ottenheijm, H.C.J.; Rees, D. Tetrahedron 1996, 52(13), 4527-4554.
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Tetrahedron
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Hermkens, P.H.H.1
Ottenheijm, H.C.J.2
Rees, D.3
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5
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0010416966
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US Pat 5,462,940
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(b) Yu, C.-N.; Pelosi, S.S.; Calcagno, M.A. US Pat 5,462,940;
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Yu, C.-N.1
Pelosi, S.S.2
Calcagno, M.A.3
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6
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0029968691
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(c) Barraclough, P.; Bolofo, M.L.; Giles, H.; Gillam, J.; Harris, C.J.; Kelly, M.G.; Leff, P.; McNeill, A.; Robertson, A.D.; Stepney, R.J.; Whittle, B.J.R. Biorg. Med. Chem. 1996 (4), 81-90.
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Barraclough, P.1
Bolofo, M.L.2
Giles, H.3
Gillam, J.4
Harris, C.J.5
Kelly, M.G.6
Leff, P.7
McNeill, A.8
Robertson, A.D.9
Stepney, R.J.10
Whittle, B.J.R.11
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7
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0029872808
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3. (a) General reference: Kline, T.; Mueller, L.; Sieber-McMaster, E.; Lau, W.F.; Meyers, C.A. Int. J. Peptide Protein Res. 1996, 47, 142-147;
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Int. J. Peptide Protein Res.
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Kline, T.1
Mueller, L.2
Sieber-McMaster, E.3
Lau, W.F.4
Meyers, C.A.5
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9
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0030842840
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(c) MMP inhibitors: Cherney, R.J.; Decicco, C.P.; Nelson, D.J.; Wang, L.; Meyer, D.T.; Hardman, K.D.; Copeland, R.A.; Arner, E.C. Biorg. Med. Chem. Lett. 1997, 7, 1757-1762;
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Cherney, R.J.1
Decicco, C.P.2
Nelson, D.J.3
Wang, L.4
Meyer, D.T.5
Hardman, K.D.6
Copeland, R.A.7
Arner, E.C.8
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10
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0028237543
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(d) Semicarbazone as a peptidomimetic group: Limal, D.; Grand, V.; Vanderesse, R.; Marraud, M. Tetrahedron Lett. 1994, 35, 3711-3714.
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Limal, D.1
Grand, V.2
Vanderesse, R.3
Marraud, M.4
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11
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0027202613
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4. There are currently five solid phase based hydantoin routes that utilize cyclizative cleavage: (a) Dewitt, S.H.; Kiely, J.S.; Stankovic, C.J.; Schroeder, M.C.; Reynolds Cody, D.M.; Pavia, M.R. Proc. Natl. Acad. Sci. 1993, 90, 6909-6913;
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Dewitt, S.H.1
Kiely, J.S.2
Stankovic, C.J.3
Schroeder, M.C.4
Reynolds Cody, D.M.5
Pavia, M.R.6
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12
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0030034999
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(b) Dressman, B.A.; Spangle, L.A.; Kaldor, S.W. Tetrahedron Lett. 1996, 37, 937-940;
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Tetrahedron Lett.
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Dressman, B.A.1
Spangle, L.A.2
Kaldor, S.W.3
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14
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0030976794
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(d) Kim, S.W.; Ahn, S.Y.; Koh, J.S.; Lee, J.H.; Ro, S.; Cho, H.Y. Tetrahedron Lett. 1997, 38, 4603-4606;
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Tetrahedron Lett.
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Kim, S.W.1
Ahn, S.Y.2
Koh, J.S.3
Lee, J.H.4
Ro, S.5
Cho, H.Y.6
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16
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0030072545
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5. Amine displacements on alpha-bromo resin esters: Scott, B.O.; Siegmund, A.C.; Marlowe, C.K.; Pei, Y.; Spear, K.L. Molecular Diversity 1995, 1, 125-134.
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Molecular Diversity
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Scott, B.O.1
Siegmund, A.C.2
Marlowe, C.K.3
Pei, Y.4
Spear, K.L.5
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17
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0025338421
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1=Me, Et, i-Bu, i-Pr, Bn) using the method according to Hoffman, R.V.; Kim, H.-O. Tetrahedron Lett. 1990, 31, 2953-2956. This gives the option of introducing chirality at the alpha carbon, however racemic starting materials were utilized in each case.
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Tetrahedron Lett.
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Hoffman, R.V.1
Kim, H.-O.2
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18
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0030061507
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7. Spatola, A.F.; Darlak, K.; Romanvskis, P. Tetrahedron Lett. 1996, 37, 591-594.
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Tetrahedron Lett.
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Spatola, A.F.1
Darlak, K.2
Romanvskis, P.3
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21
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0010337505
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note
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2: C, 50.6; H, 4.98; N, 18.38. Found: C, 50.1; H, 4.73; N, 17.9.
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22
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0010384793
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note
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11. For entry 13, phenyl alanine was utilized as the silylated (TMS) ester by first heating the acid in bis(trimethylsilyl)acetamide (BSA, 3 equiv., DMF, 80°C), followed by cooling to room temperature, and then addition of the solution directly to the resin (step h, Scheme 1). Also, DMAP was used in place of DIPEA.
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