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报道通过延伸方法解决季戊四醇(1)及三羟甲基氨甲烷(2)末端羟基立体位阻的方法。(1)和(2)末端羟基经氰乙基化、醇解和还原等步骤制得标题化合物四(ω-羟丙氧甲基)甲烷(3)及三(ω-羟丙氧甲基)氨甲烷(4),并合成9个衍生物,以摸索(3)和(4)的酰化、醚化及氯化等反应条件。所合成的化合物(3~13)及(15)均未见文献报道,其结构经IR、1H-NMR和元素分析确证。标题化合物可作为小分子多功能桥试剂,以增大载体的载药量。
A method for solving the steric hindrance of pentaerythritol (1) and trimethylolaminomethane (2) at the terminal hydroxyl group by an extension method is reported. (Ω-hydroxypropoxymethyl) methane (3) and tris (ω-hydroxypropoxymethyl) methane were subjected to steps of cyanoethylation, alcoholysis and reduction at the terminal hydroxyl groups of (1) and Ammonia methane (4) was synthesized and nine derivatives were synthesized to explore the reaction conditions of acylation, etherification and chlorination of (3) and (4). The synthesized compounds (3 ~ 13) and (15) have not been reported in the literature. Their structures were confirmed by IR, 1H-NMR and elemental analysis. The title compound can be used as a small molecule multifunctional bridging agent to increase the carrier drug loading.