A.N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, Vavilov str. 28, 119991, Moscow, Russia.
J Org Chem. 2012 Oct 5;77(19):8518-26. doi: 10.1021/jo301501r. Epub 2012 Sep 14.
An efficient method for the synthesis of novel CF(3)-substituted tetrahydro-1,7-naphthyridines including cyclic α-amino acid derivatives has been developed. The method is based on unusual cyclobutene ring-opening of bicyclo[4.2.0]octa-1,6-dienes with pyrrolidine to afford the corresponding 1,5-diketones followed by their heterocyclization. A convenient one-pot procedure has been also elaborated starting from readily available trifluoromethylated 1,6-allenynes.
一种高效的合成新型 CF(3)-取代的四氢-1,7-萘啶的方法，包括环状α-氨基酸衍生物，已经被开发出来。该方法基于双环[4.2.0]辛-1,6-二烯与吡咯烷的不寻常的环丁烯开环反应，生成相应的 1,5-二酮，然后进行杂环化。从易得的三氟甲基化 1,6-烯炔出发，还详细阐述了一种方便的一锅法。
