Pyridazine derivatives.: Part 38:: Efficient Heck alkenylation at position 5 of the 6-phenyl-3(2H)-pyridazinone system

被引:22
作者
Coelho, A
Sotelo, C
Novoa, H
Peeters, OM
Blaton, N
Raviña, E
机构
[1] Univ Santiago de Compostela, Fac Farm, Quim Farmaceut Lab, Dept Quim Organ, Santiago De Compostela 15782, Spain
[2] Katholieke Univ Leuven, Fac Farmaceut Wetenschappen, Lab Analyt Chem Med Fysicochem, B-3000 Louvain, Belgium
关键词
pyridazinones; Heck coupling; phthalazinones;
D O I
10.1016/j.tetlet.2004.03.005
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Several 6-phenyl-3(2H)-pyridazinones bearing different alkenyl groups at position 5 have been prepared in the search for novel antiplatelet agents. The target compounds were synthesised by a palladium-catalysed Heck cross-coupling reaction. Variable amounts of 4-phenyl-6-substituted-2-phthalazinones were isolated as by-products during these experiments. The crucial issues for successful Heck coupling in these systems concern the protection of position 2 of the heterocyclic ring and the use of tris(o-tolyl)phosphine as a ligand. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3459 / 3463
页数:5
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