反应详情

温度

120 °C

The preparation was carried out analogously to Example 86, using 0.125 g (0.308 mmol) N-(5-iodopyridin-2-yl)-N′-(2-methoxybenzyl)guanidine, 0.055 g (0.431 mmol) 2-thienylboric acid, 0.098 g (0.925 mmol) sodium carbonate, and 0.018 g (0.015 mmol) tetrakis-(triphenylphosphine)-palladium(0). The mixture was likewise heated for 60 min at 120° C. in a CEM microwave (200 watts). After filtration and purification via preparative HPLC, 23 mg N-(2-methoxybenzyl)-N′-[5-(2-thienyl)pyridin-2-yl]guanidine was isolated, a small portion of which was present in the form of the acetate salt (base/acetate in a ratio of 1:0.3).

1. filtrationAfter filtration and purification via preparative HPLC