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Solution-phase library synthesis
Solution-phase library synthesis O 0357Solution-Phase Parallel Synthesis of 4,6-Diaryl-pyrimidine-2-ylamines and 2-Amino-5,5-disubstituted-3,5-dihydro-imidazol-4-ones via a Rearrangement. -Imidazoles are formed by reaction of 1,3-diarylpropenones with guanidine in the presence of hydrogen peroxide. A stepwise reaction of 1,3-diarylpropenones first with guanidine and then with hydrogen peroxide affords pyrimidines. The formation of the imidazoles is apparently the result of a rearrangement with migration of the aryl ring in the proximity of the carbonyl group of the propenones. Based on these reactions, libraries of type (III) and (V) or (VI) and (VII) together with some N-acyl derivatives are prepared in solution phase parallel synthesis utilizing a cascade matrix technology. The yields generally vary in the range of 30 to 70%. -(VARGA, L.; NAGY, T.; KOEVESDI, I.; BENET-BUCHHOLZ, J.; DORMAN, G.; UERGE, L.; DARVAS*, F.; Tetrahedron 59 (2003) 5, 655-662; ComGenex Inc., H-1388 Budapest, Hung.; Eng.) -Klein 21-075
The physicochemical properties of the novel compounds such as (III), (V) and (VII) are assessed and the results are discussed. -(SZABO, D.; BONTO, A.-M.; KOEVESDI, I.; GOEMOERY, A.; RABAI*, J.; J. Fluorine Chem. 126 (2005) 4, 641-652; Dep. Org. Chem., Eoetvoes Lorand Univ., H-1518 Budapest, Hung.; Eng.) -K. Schneider 40-082
O‐acetyl derivatives of the phthalazinones (I) and (VII) undergo proton‐catalyzed ring‐closure reactions in the melt to give the title ring systems (III) and (VIII), respectively.
On Triazoles. Part 35. The Reaction of 5-Amino-1,2,4-triazoles with Di-and Triketones.--(REITER, J.; PONGO, L.; KOEVESDI, I.; PALLAGI, I.; J. Heterocycl. Chem. 32 (1995) 2, 407-417; EGIS Pharm., H-1475 Budapest, Hung.; EN)
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