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以邻羧基苯甲醛为初始原料,经Wittig-Horner反应,环合,水解,酸化得到奥拉帕尼重要中间体2-氟-5-[(4-氧代-3 H-2,3-二氮杂萘基)甲基]苯甲酸,总收率为75.3%,较文献[8-13]提高12%。各步关键中间体及目标物结构经MS和~1H NMR确证。改进后的工艺操作简便,成本降低,工业化生产的市场竞争优势更大。
The ortho-carboxybenzaldehyde was used as the starting material to obtain 2-fluoro-5 - [(4-oxo-3H- Naphthyridinyl) methyl] benzoic acid in 75.3% yield, which is 12% higher than that of [8-13]. The key intermediates and target structures of each step were confirmed by MS and ~ 1H NMR. The improved process is simple and easy to operate, the cost is reduced, and the market competitive advantage of industrialized production is even greater.