原创力文档synthesis of a new scaffold the 7h,8h-pyrimido[1,6-b]pyridazin-6,8-dione nucleus合成一个新的支架7 h,8 h-pyrimido[1,6 b]pyridazin-6 8-dione细胞核.pdfVIP
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synthesis of a new scaffold the 7h,8h-pyrimido[1,6-b]pyridazin-6,8-dione nucleus合成一个新的支架7 h,8 h-pyrimido[1,6 b]pyridazin-6 8-dione细胞核
Molecules 2007, 12, 2643-2657
molecules
ISSN 1420-3049
© 2007 by MDPI
/molecules
Full Paper
Synthesis of a New Scaffold:
the 7H,8H-Pyrimido[1,6-b]pyridazin-6,8-dione Nucleus
Franciszek Herold 1,*, Małgorzata Kałucka 1, Marek Król 1, Joanna Herold 2, Jerzy Kleps 1 and
1
Jadwiga Turło
1 Department of Drug Technology, Faculty of Pharmacy, Medical University of Warsaw, Banacha 1
Str., 02-097 Warsaw, Poland
2 Department of Drug Chemistry, Faculty of Pharmacy, Medical University of Warsaw, Banacha 1
Str., 02-097 Warsaw, Poland
* Author to whom correspondence should be addressed; E-mail: herold@.pl
Received: 6 December 2007; in revised form: 21 December 2007 / Accepted: 21 December 2007/
Published: 30 December 2007
Abstract: This paper describes a modified method of preparation of a number of α-aryl-α-
(pyridazin-3-yl)-acetonitriles via the C-arylation reaction of the corresponding carbanions
of phenylacetonitriles using 3-chloropyridazine derivatives. KOH and DMSO were used in
the deprotonation process, which made the reaction very simple and safe to perform.
Nitriles were obtained in the hydrolysis reaction to the corresponding α-aryl-α-(pyridazin-
3-yl)-acetamide derivatives, which were next subjected to cyclization to afford the final
products. A number of new derivatives of 7H,8H-pyrimido[1,6-b]pyridazin-6,8-dione were
synthesized in the cyclocondensation reaction of respective α-aryl-α-(pyridazin-3-yl)-
acetamides with diethyl carbonate in t
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