Top Abstract Purchase Related
Home
>
Node
>
Subnode

Automated synthesis of heterocycles on solid supports

Jung, N.; Encinas, A.; Bräse, S.

Current Opinion in Drug Discovery and Development 9(6): 713-728

2006

ISSN/ISBN: 1367-6733
PMID: 17117682
Document Number: 602332
The creation of novel diverse heterocycle libraries is an indispensable requirement of modern drug discovery processes. Currently, library sizes of over 10,000 discrete compounds are viable using programmed synthesis on solid supports. This review discusses the recent advances in the automated solid-phase syntheses of heterocycles to generate libraries of bioactive products, and illustrates library sizes that have been obtained, robots used for production of libraries, points of diversity and number of steps on the resin.

Document emailed within 1 workday
Secure & encrypted payments

Vu, H.; Singh, P.; Joyce, N.; Hogan, M.E.; Jayaraman, K. 1993: Synthesis of cholesteryl supports and phosphoramidites containing a novel peptidyl linker for automated synthesis of triple-helix forming oligonucleotides (TFOs) Nucleic Acids Symposium Series 29: 19-20
Vu, H.; McCollum, C.; Lotys, C.; Andrus, A. 1990: New reagents and solid support for automated oligonucleotide synthesis Nucleic Acids Symposium Series 22: 63-64
Kates, S.A.; Solé, N.A.; Beyermann, M.; Barany, G.; Albericio, F. 1996: Optimized preparation of deca(L-alanyl)-L-valinamide by 9-fluorenylmethyloxycarbonyl (Fmoc) solid-phase synthesis on polyethylene glycol-polystyrene (PEG-PS) graft supports, with 1,8-diazobicyclo [5.4.0]-undec-7-ene (DBU) deprotection Peptide Research 9(3): 106-113
Baru, M.B.; Cherskiĭ, V.V.; Danilov, A.V.; Moshnikov, S.A.; Mustaeva, L.G. 1995: The automated "SynChrom" system for solid-phase synthesis of peptides and liquid column chromatography. II. use in the solid-phase synthesis of peptides and liquid column chromatography Bioorganicheskaia Khimiia 21(7): 506-516
Metwally, M.A.; el-Hussiny, M.S.; el-Ablak, F.Z.; Khalil, A.M. 1989: Synthesis of some heterocycles of pharmaceutical interest Die Pharmazie 44(4): 261-265
Muylaert, K.; Jatczak, M.; Mangelinckx, S.; Stevens, C.V. 2014: Synthesis Of Pyrido-Annelated Seven-Membered N-Containing Heterocycles Current Medicinal Chemistry 2014
Zuo, Z.-z.; Zhong, H.; Cai, T.; Bao, Y.; Liu, Z.-q.; Liu, D.; Zhao, L.-x. 2015: Design, synthesis and antiproliferative activities of artemisinin derivatives substituted by N-heterocycles Yao Xue Xue Bao 50(7): 868-874
Alcaide, B.; Almendros, P.; Aragoncillo, C. 2010: Highly reactive 4-membered ring nitrogen-containing heterocycles: Synthesis and properties Current Opinion in Drug Discovery and Development 13(6): 685-697
Metwally, M.A.; el-Hossini, M.S.; el-Ablak, F.Z.; Khalil, A.M. 1992: Synthesis of condensed heterocycles from 3-aryl-2,4-dicarbethoxy-5-methylcyclohexanones and their testing for antimicrobial activity Die Pharmazie 47(5): 336-339
Mikhaĭlitsyn, F.S.; Kozyreva, N.P.; Rabinovich, S.A.; Maksakovskaia, E.V.; Kulikovskaia, I.M.; Dadasheva, N.R.; Lebedeva, M.N.; Bekhli, A.F.; Lychko, N.D.; Uvarova, N.A. 1992: The search for new antiparasitic agents. 10. the synthesis, toxicological and antimalarial properties of nitrogen-containing heterocycles with a 4-(4-alkylpiperazinyl-1) phenylamine substituent (the preparation quinoprazine) Meditsinskaia Parazitologiia i Parazitarnye Bolezni 1: 50-53
Curran, D.P. 1998: Fluorous synthesis: an alternative to organic synthesis and solid phase synthesis for the preparation of small organic molecules Cancer Journal from Scientific American 4(Suppl 1): S73-S76
Grandolini, G.; Ambrogi, V.; Perioli, L.; Giannaccini, G.; Lucacchini, A.; Martini, C. 1996: Studies on annelated 1,4-benzothiazines and 1,5-benzothiazepines. X--Synthesis and inhibition of benzodiazepine receptor binding of new 1,4-thiazine and 1,5-thiazepine polycondensed heterocycles with steroidal structure Farmaco 51(3): 203-207
Miyoshi, K.; Itakura, K. 1980: Solid-phase synthesis of polynucleotides: V. Synthesis of oligodeoxyribonucleotides by the phosphomonotriazolide method Nucleic Acids Symposium Series 7: 281-291
Fujii, M.; Nagai, H.; Sekine, M.; Hata, T. 1986: The phosphorothioite method. Synthesis of deoxyoligonucleotides on polymer supports by using nucleoside phosphorothioites Nucleic Acids Symposium Series 17: 77-80
Reddy, B.S. 1989: Biologically active polymer supports based on cellulosic derivatives: synthesis and kinetic study Indian Journal of Biochemistry and Biophysics 26(2): 80-83
Gait, M.J.; Popov, S.G.; Singh, M.; Titmas, R.C. 1980: Rapid synthesis of oligodeoxyribonucleotides. V. Further studies in solid phase synthesis of oligodeoxyribonucleotides through phosphotriester intermediates Nucleic Acids Symposium Series 7: 243-257
Ling, N.; Esch, F.; Davis, D.; Mercado, M.; Regno, M.; Bohlen, P.; Brazeau, P.; Guillemin, R. 1980: Solid phase synthesis of somatostatin-28 Biochemical and Biophysical Research Communications 95(3): 945-951
Sabirov, A.; Lyu, R.-M.; Chen, X.-Q.; Tian, Q.; Chang, J.-K. 2013: A total solid-phase synthesis of DILP8 Italian Journal of Anatomy and Embryology 118(1 Suppl): 13-14
Guitton, J.; Durand, D.; Bouillod, N.; Manchon, M. 1994: Development of a solid/liquid extraction method for analysis of toxic drugs in serum using an automated liquid chromatograph: the Remedi Annales de Biologie Clinique 52(2): 111-115
Cech, D.; Schubert, F.; Möller, U. 1991: Non-radioactive labelling of oligonucleotides with pre-functionalized phosphoramidites or H-phosphonates during automated synthesis Nucleic Acids Symposium Series 24: 205-206