A New Approach to Polycyclic Azonia Cations by Ring-Closing Metathesis Ana Nu ´n ˜ ez, Ana M. Cuadro,* Julio Alvarez-Builla, and Juan J. Vaquero* Departamento de Quı ´mica Orga ´ nica, UniVersidad de Alcala ´ , 28871-Alcala ´ de Henares, Madrid, Spain juanjose.Vaquero@uah.es Received March 30, 2007 ABSTRACT The ring-closing metathesis (RCM) reaction of N-vinyl-r-(2-styryl)azinium salts, using the Hoveyda-Grubbs catalyst, leads to different tricyclic and tetracyclic azonia cations with moderate to good yields. This is the first time that a highly electron-deficient alkene such as an N-vinylpyridinium has been involved in an RCM process. Recently, we reported the first examples of a diene 1 and enyne 2 ring-closing metathesis on azinium cations 1, a pro- cess that gave dihydroquinolizinium cations 2. This strategy proved to be very efficient for the synthesis of quinolizinium derivatives and related systems 3,4 (Scheme 1). Indeed, it can be envisaged as a unified approach to a range of azonia cations, 5 including the 3 benzoquinolizinium and many of the 18 possible dibenzo- and naphthoquinolizinium cations. 6 There are, however, a small number of dibenzo- and naphthoquinoliziniums (4-6) for which this strategy, based on the disconnection of the δ bond with respect to the quaternary nitrogen, is not feasible because the presence of two benzo fused rings precludes the appropriate bond disconnection. For this class of cations, which includes the dibenzo[a,g]quinolizinium cation 6 (the heterocyclic core of cationic alkaloids such as coralyne, 7 berberine, and proto- berberines 8 ), we envisaged an alternative diene ring-closing metathesis (RCM) process through the disconnection of a bond (Scheme 2). Dedicated to Prof. Miguel Yus on the occasion of his 60th birthday. (1) For recent reviews on diene RCM, see: (a) Deiters, A.; Martin, S. F. Chem. ReV. 2004, 104, 2199-2238. (b) Poulsen, C. S.; Madsen, R. Synthesis 2003,1-18. (c) Trnka, T. M.; Grubbs, R. H. Acc. Chem. Res. 2001, 34, 18-29. (2) For reviews on enyne metathesis, see: (a) Fu ¨rstner, A.; Davies, P. W. Chem. Commun. 2005, 2307-2320. (b) Hoveyda, A. H.; Hird, A. W.; Kacprzynski, M. A. Chem. Commun. 2004, 1779-1785. (c) Diver, S. T.; Giessert, A. J. Chem. ReV. 2004, 104, 1317-1382. (d) Mori, M. In Handbook of Metathesis; Grubbs, R. H., Ed.; Wiley-VCH: Weinheim; Germany, Vol. 2003; Vol. 2, 176-204. (e) Mori, M. Top. Organomet. Chem. 1998, 1, 133-154. (3) Nun ˜ez, A.; Cuadro, A. M.; Alvarez-Builla, J.; Vaquero, J. J. Org. Lett. 2004, 6, 4125-4127. (4) Nun ˜ez, A.; Cuadro, A. M.; Alvarez-Builla, J.; Vaquero, J. J. Chem. Commun. 2006, 2690-2692. (5) Ihmels, H.; Faulhaber, K.; Vedaldi, D.; Dall’Acqua, F.; Viola, G. Photochem. Photobiol. 2005, 81, 1107-1115. (6) Arai, S.; Hida, M. AdV. Heterocycl. Chem. 1992, 55, 261-358. (7) (a) Kwang-Yuen, K.-Y.; Zee-Cheng, Y.; Paul, K. D.; Cheng, C. C. J. Med. Chem. 1974, 17, 347-351. (b) Robert, K.; Zee-Cheng, Y.; Cheng, C. C. J. Med. Chem. 1976, 19, 882-886. (c) Wilson, W. D.; Gough, A. N.; Doyle, J. J.; Davidson, M. W. J. Med. Chem. 1976, 19, 1261-1263. (d) Lee, J. S.; Latimer, L. J. P.; Hampel, K. J. Biochemistry 1993, 32, 5591- 5597. (e) Wang, L.-K.; Rogers, B. D.; Hecht, S. M. Chem. Res. Toxicol. 1996, 9, 75-83. Scheme 1. 3,4-Dihydroquinolizinium from δ Bond Disconnection ORGANIC LETTERS 2007 Vol. 9, No. 16 2977-2980 10.1021/ol070773t CCC: $37.00 © 2007 American Chemical Society Published on Web 07/11/2007