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1.15 References [1] (a) William A.S., Aleksel F.B., Ron C., Organic Synthesis: the science behind art. Royal Society of Chemistry (Great Britain). (b) Organic Synthesis Coll vol. and (c) Comprehensive organic Synthesis book volumes. [2] For recent reviews on microwave-assisted organic synthesis see: (a) Kappe, C. O. (2004) Angew.Chem.Int.Ed., 43, 6250. (b) Kappe, C. O., Dallinger, D. (2006) Nat. Drug. Disc. Rev., 5, 51. (c) Nagariya A.K., Meena.A.K., Kiran, Yadav A.K., Niranjan.U.S., Pathak A.K., Singh. B., Rao.M.M. (2010) Journal of pharmacy Research. 3, 575-580. (d) Jignasa.K.S. Ketan T.S., Bhumika.S.P., Anuradha K.G., (2010) Der Pharma Chemica, 2, 1, 342-353. [3] (a) Adam, D. (2003) Nature, 421, 571-572. (b) Blackwell, H. E. (2003) Org. Biomol. Chem. 1, 1251-55. [4] Sharma, S. V.; Rama-sarma, G. V. S.; Suresh, B. (2002), Indian. J. Pham. Scien. 64, 337-344. [5] Johansson, H. (2001) Am. Lab. 33, 10, 28-32. [6] Bradley, D. (2001) Modern Drug Discovery 4, 32-36. [7] Larhed, M.; Hall berg, A. (2001) Drug Discovery Today. 6, 406-416. [8] Wathey, B.; Tierney, J.; Lidrom, P.; Westman, (2002) J. Drug Discovery Today, 7, 373-380. [9] Dzieraba, C. D.; Combs, A. P. (2002) Annual reports in medicinal chemistry, academic press, 37, 247-256. [10] In; http://www.milestonesci.com. [11] In; http://www.maos.net. [12] In; http://www.cem.com. [13] Westaway, K. C.; Gedye, R. J. (1995) Microwave Power Electromagnetic energy 30, 219- 230. [14] Kuhnert, N. (2002) Angrew Chem. Int. Ed. 41, 1863-1866. [15] Gabriel, C.; Gabriel, S.; Grant, E. H.; Holstead, B. S. T.; Mingos, D. M. P. (1998) Chem. Soc. Rev. 27, 213-23. [16] Langa, F.; DelaCruz, P.; DelaHoz, A.; Diaz-Ortiz, A.; Diez-Barra, E. (1997) Org. Synth. 4, 373-86. [17] Saillard, R.; Poux, M.; Berlan, J.; Audhvy-peaudecert, M. (1995) Tetrahedron, 51, 4033-42. [18] Stuerga, D.; Gaillard, P. (1996) Tetrahedron 52, 5505-10. [19] Caddick, S. (1995) Tetrahedron 51, 10403-32. [20] Strauss, C. R.; Trainor, R. W. (1995) Aust. J. Chem. 48, 1665-1692. [21] Bose, A. K.; Banik, B. K.; Lavlinskaia, N.; Jayaraman, M.; Manhas, M. S. (1997) Chemtech. 27, 18-124. [22] Lidstrom, P.; Tierney, J.; Wathey, B.; Westman, J. (2001) Tetrahedron, 57, 9225-83. [23] Nuchter. M.; Ondruschka, B.; Lautenschlager, W. (2003) Chem. Eng. Techno. 26, 1208- 1216. [24] Nuchter. M.; Ondruschka, B.; Bonrath, W.; Gum, A. (2004) Green Chem. 6, 128-141. [25] Abramovitch, R. A. (1991), Org. Prep. Proced. Int. 23, 685-711.
[26] Leadbeater, N. E. (2004) Chemistry World 1, 38-41. [27] Moghaddam, F. M.; Sharifi, A. (1995) Synth. Commun. 25, 2457-61. [28] Mogilaiah, K.; Kavita, S.; Babu, H. R. (2003) Indian J. Chem. 42b, 1750-52. [29] Abramovitch, R. A.; Shi, Q.; Bogdal, D. (1995) Synth. Commun. 25, 1-8. [30] Miljanic, O. S.; Volhardt, K. P. C.; Whitener, G. D. (2003) Synlett. 1, 29-34. [31] Motorina, I. A.; Parly, F.; Grierson, D. S. (1996) Synlett. 4, 389-91. [32] Mccarroll, A. J.; Sandham, D. A.; Titumb, L. R.; Dek Lewis, A. K.; Cloke, F. G. N.; Davies, B. P.; Desantand, A. P.; Hiller, W.; Caddicks, S. (2003) Molecular Diversity 7, 115-23. [33] Robeiro, G. L.; Khandikar, B. M. (2003) Synth. Commun. 33, 10405-10. [34] Wali, A.; Paillai, S. M.; Satish, S. (1995) Indian petrochemical Corp. Ltd. 294. [35] Yamazaki, K.; Kondo, V. (2003) J. Comb. Chem., 5, [36] Al-obeidi, F.; Austin, R. E.; Okonoya, J. F.; Bond, D. R. S. Mini-rev. (2003) Med. Chem. 3, 449. [37] Kim, J. K.; Kwon, P. S.; Kwon, T. W.; Chung, S. K.; Lee, J. W. (1996) Synth. Commun. 26, 535-42. [38] Burten, G.; Cao, P.; Li, G.; Rivero, R. (2003) Org. Lett. 5, 4373-76. [39] Arevela, R. K.; Leadbeater, N. E. (2003) J. Org Chem. 68, 9122-25. [40] Crawford, K. R.; Bur, S. K.; Straub, C. S.; Padwa, A. (2003) Org. Lett. 5, 3337-40. [41] Lerestif, J. M.; Perocheav, J.; Tonnard, F.; Bazareav, J. P.; Hamelin, J. (1995) Tetrahedron 51, 6757-74. [42] Jaya Kumar, G.; Ajithabai, M. D.; Santhosh, B.; Veena, C. S.; Nair, M. S. (2003) Indian J. Chem. 42B, 429-31. [43] Calinescu, I.; Calinescu, R.; Martin, D.I.; Radoiv, M. T. (2003) Res. Chem. Inter med. 29, 71- 81. [44] Mavoral, J. A.; Cativicla, C.; Garcia, J. I.; Pires, E.; Rovo, A. J.; Figueras, F. (1995) Appl. Catal. 131, 159-66. [45] Santagoda, V.; Fiorino, F.; Perissuti, E.; Severino, B.; Terracciano, S.; Cirino, G.; Caliendo, G. (2003) Tetrahedron lett. 5, 2131-34. [46] Roy, I.; Gupta, M. N. (2003) Tetrahedron Lett. 44, 1145-48. [47] Diaz-Ortiz, A.; Dela Hoz, A.; Merrero, M. A.; Prieto, P.; Sanchez-Migallon, A.; Cassio, F. P.; Arriela, A.; Vivanco, S.; Foces, C. (2003) Molec. Divers. 7, 165-69. [48] Jnagaki, T.; Fukuhara, T.; Hara, S. (2003) Synthesis 8, 1157-59. [49] Plazl, I.; Leskovesek, S.; Kolooini, T. (1995) Chem. Eng. J. 59, 253-57. [50] Lechmann, F.; Pilotti, A.; Luthman, K. (2003) Molec. Divers. 7, 145-52. [51] Kiasat, A. R.; Kazemi, F.; Rastogi, S. (2003) Synth. Commun. 33, 601-06. [52] Gospondinova, M.; Gredard, A.; Jeannin, M.; Chitanv, G. C.; Carpov, A.; Thiery, V.; Besson, T. (2002) Green chem. 4, 220-22. [53] Vu, z. T.; Liu, L. J.; Zhuo, R. X. (2003) Polym. Chem. Ed. 41, 13-21. [54] Srikrishana, A.; Kumar, P.P. (1995) Tetrahedron Lett. 36, 6313-16. [55] Chattopadhyay, S.; Banerjee, S.K.; Mitra, A.K. (2002) J. Indian Chem. Soc. 79, 906-907.
Page 1 and 2: Saurashtra University Re - Accredit
Page 3: JANUARY-2011 Statement under O. Ph.
Page 7 and 8: Acknowledgment This thesis arose in
Page 9 and 10: since I was a child. My Mother Hans
Page 11 and 12: CHAPTER - 2 Microwave Assisted Synt
Page 13 and 14: 5.5 Results and discussion 156 5.6
Page 15 and 16: Ms Mesyl MW Microwave NBS N-bromosu
Page 17 and 18: 1. Microwave Assisted Organic Synth
Page 19 and 20: 1.4 Heating Mechanism In microwave
Page 21 and 22: 1.5. Effects of solvents Every solv
Page 23 and 24: 1.7 Application of microwave in org
Page 25 and 26: aromatic amines, Lancini’s group
Page 27 and 28: 1.9 2-Aminoimidazole Alkaloids The
Page 29 and 30: Recently group of Erik 83 described
Page 31 and 32: 1.10 Methods for the preparation of
Page 33 and 34: R 1 O X R 2 NH 2 H 2N NAc R 1 HN R
Page 35 and 36: this manifold, was reported in 1925
Page 37 and 38: Another route to 4(5)-acyl-2-amino-
Page 39 and 40: this series of compounds against th
Page 41 and 42: documented. Extra care is needed be
Page 43 and 44: Very recently the research group of
Page 45 and 46: OH a,b O N H2N N Boc N 3 H N R N N
Page 47 and 48: 1.12.2 Biofilm Growth Cycle 1) Plan
Page 49: can survive both the onslaught of a
Page 53 and 54: [86] Kreutzberger, A. (1962) J. Org
Page 55 and 56: Microwave Assisted Synthesis & Stru
Page 57 and 58: 2.1 Introduction As described in ch
Page 59 and 60: 2.3 Proposed Mechanism: Regarding t
Page 61 and 62: No. 12 60 120 traces 84 a All react
Page 63 and 64: the development of biofilm related
Page 65 and 66: In first instance, a series of 2-hy
Page 67 and 68: Br N N N R 1 OH Br N N N R 1 OH Fig
Page 69 and 70: do have a very strong effect agains
Page 71 and 72: 2.6 Conclusion In the present study
Page 73 and 74: 2.8 Biological assays 2.8.1 Static
Page 75 and 76: 2.9 Experimental protocol: 2.9.1 Ge
Page 77 and 78: temperature of 80 °C and a maximum
Page 79 and 80: 29.5,29.4, 29.2, 27.0, 22.6, 14.1.
Page 81 and 82: Yield: 78 %. 1 H NMR (300 MHz, CDCl
Page 83 and 84: N Br N N C 14H 29 OH Yield: 72 %. 1
Page 85 and 86: (75.5 MHz, CDCl3): δ = 167.7, 154.
Page 87 and 88: N Br N N C 14H 29 OH Cl Yield: 90 %
Page 89 and 90: 2-(3,4-Dichlorophenyl)-2-hydroxy-1-
Page 91 and 92: N Br N N C 8H 17 OH NO 2 Yield: 49
Page 93 and 94: C3H7 HN N N H Cl Cl Yield : 70 %. 1
Page 95 and 96: (s, 1H), 3.16 (s, 3H), 1.80 (m, 2H)
Page 97 and 98: 5-(4’-Nitrobiphenyl-4-yl)-N-octyl
Page 99 and 100: 2.11 Representative NMR spectra 2.1
Page 101 and 102:
2.11.3 10.4329 0.7429 151.5720 10.0
Page 103 and 104:
[21] Matz C, McDougald D, Moreno A.
Page 105 and 106:
Chapter-3 Structure Activity Relati
Page 107 and 108:
imidazoles, where the addition of a
Page 109 and 110:
3.4 Result and Discussion It was fo
Page 111 and 112:
No. H 2N Compound Code N N C8H17 R1
Page 113 and 114:
medium used in the set-up to monito
Page 115 and 116:
H 2N N N N H2N N R R Figure-1 Effec
Page 117 and 118:
3.5.3 Cyclo-alkyl 2-aminoimidazoles
Page 119 and 120:
3.6. Conclusion In the present stud
Page 121 and 122:
3.8. Experimental protocols 3.8.1 G
Page 123 and 124:
122.6, 54.6, 33.3(×2), 27.3 (×2),
Page 125 and 126:
Yield: 52 %. 1 H NMR (300 MHz, CDCl
Page 127 and 128:
5-(4-Chlorophenyl)-1-cyclooctyl-1H-
Page 129 and 130:
Yield: 50 %. Mp: 76-78 ° C. 1 H NM
Page 131 and 132:
5-(4-Chlorophenyl)-1-cyclobutyl-1H-
Page 133 and 134:
Yield: 66%. 1 H NMR (300 MHz, CDCl3
Page 135 and 136:
3.10 Representative NMR spectra 3.1
Page 137 and 138:
3.11 References [1] (a) Alvi K. A,
Page 139 and 140:
Copper Catalyzed Microwave Assisted
Page 141 and 142:
4.1 Introduction There are only a f
Page 143 and 144:
(Table-1, No- 6). Next reaction tem
Page 145 and 146:
No. Product, Yield b (%) No. Produc
Page 147 and 148:
4.4 Possible Mechanism Regarding th
Page 149 and 150:
4.7 Experimental protocols 4.7.1 Ge
Page 151 and 152:
Yield: 69 %. 1 H NMR (300 MHz, CDCl
Page 153 and 154:
1-(3-Azidopropyl)-2-(3,4-dichloroph
Page 155 and 156:
Yield: 84 %. 1 H NMR (300 MHz, DMSO
Page 157 and 158:
Page 159 and 160:
Page 161 and 162:
1H), 1.66 (m, 6H), 1.70 (m, 2H). 13
Page 163 and 164:
5.48 Hz, 2H), 3.59 (m, 2H), 3.16 (d
Page 165 and 166:
4.10 References [1] For a general r
Page 167 and 168:
Crystal and Molecular Structure Ana
Page 169 and 170:
5.1 Introduction The membrane efflu
Page 171 and 172:
oscillation range of 5˚ and proces
Page 173 and 174:
C12-C13 1.372(4) C32-C37 1.390(3) C
Page 175 and 176:
Fig.-3: Packing of the molecules wh
Page 177 and 178:
1 H NMR (400 MHz CDCl3): δ = 7.57-
Page 179 and 180:
5.9.2 13 C spectra of bs-DP-7
Page 181 and 182:
SUMMARY The work represented in the
Page 183 and 184:
CONFERENCES/SEMINARS/WORKSHOPS ATTE
Page 185:
PUBLICATIONS [1] One-Pot Microwave-
Page 200 and 201:
Scheme 2 Competitive formation of 1
Page 202 and 203:
Table 2 continued 9 10 11 12 N hydr
Page 204:
8. Colson G, Raboult L, Lavelle F,
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