Palacios Francisco, Ochoa de Retana Ana María, Gil José Ignacio, López de Munain Rafael
Facultad de Farmacia, Universidad del País Vasco, Apartado 450, 01080 Vitoria, Spain.
Org Lett. 2002 Jul 11;4(14):2405-8. doi: 10.1021/ol0261534.
[reaction: see text] Tetrasubstituted pyrazines containing two phosphonate groups 2 in positions 2 and 5 and trisubstituted pyrazines containing a phosphonate 5 or a phosphine oxide group 7 in position 2 are obtained by thermal treatment of 2H-azirine-2-phosphonates 1 and -phosphine oxides 6. These pyrazines can also be prepared from beta-ketoxime tosylates 9 and 10 or from oxime derived from phosphine oxide 11.
[反应:见正文] 通过对2H-氮丙啶-2-膦酸酯1和-膦氧化物6进行热处理,可得到在2位和5位含有两个膦酸酯基团2的四取代吡嗪以及在2位含有膦酸酯5或膦氧化物基团7的三取代吡嗪。这些吡嗪也可由β-酮肟对甲苯磺酸盐9和10或由膦氧化物11衍生的肟制备。