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目的使用不对称亨利反应合成沙美特罗。方法以4-苯基丁醇为起始原料合成长链脂肪醛,同时由对羟基苯甲醛出发经3步反应制备前手性苯甲醛,继而通过不对称亨利反应制得手性硝基醇化合物,随后用氢化方法合成(R)-沙美特罗。结果与结论通过不对称亨利反应制得硝基醇化合物,产物的对映选择性较好(60%ee),新路线省去了原文献中制备三级胺和脱苄基两步反应,合成路线未见报道。
Aim To synthesize salmeterol using the asymmetric Henry reaction. Methods 4-phenylbutanol was used as the starting material to synthesize long chain aliphatic aldehydes. Chiral benzaldehyde was prepared from p-hydroxybenzaldehyde by 3 steps and then chiral nitroalcohol was obtained by asymmetric Henry reaction. The (R) -salmeterol is then hydrogenated. RESULTS AND CONCLUSION Nitroalcohol compounds were prepared by asymmetric Henry reaction and the enantioselectivity of the products was good (60% ee). The new route omits the two-step reaction of preparing tertiary amines and debenzylation in the original literature and synthesizing Route has not been reported.