光动力化合物5-氨基乙酰丙酸的简便全合成

Simple Total Synthesis of Photodynamic Compound 5-Aminolevulinic Acid

从γ-丁内酯出发,首先发生醇解、氧化反应,继而采用无溶剂法与硝基甲烷在KF/Al2O3催化下发生Henry反应,再经湿Al2O3负载的CrO3氧化得到5-硝基-4-羰基戊酸乙酯,最后在Pd/C催化下还原得到5-氨基乙酰丙酸.各步所合成化合物的结构经1HNMR,IR,MS分析确证.

5-Aminolevulinic acid （5-ALA） was prepared from γ-butyrolactone via alcoholysis, oxidation, Henry reaction, oxidation and hydrogenation. Especially Henry reaction was carried out through a solvent-free procedure in the presence of alumina supported potassium fluoride, and then oxidation of the nitroalkanol was finished using wet alumina supported chromium（Ⅵ） oxide. The structures of all the compounds were confirmed by ^1H NMR, IR and MS spectra.