In order to construct the zwitterionic structure of phosphorylcholine onto the surface of biomaterials, five novel phospholanes containing hydroxyl group were synthesized from the corresponding diol and 2-chloro-2-oxo...In order to construct the zwitterionic structure of phosphorylcholine onto the surface of biomaterials, five novel phospholanes containing hydroxyl group were synthesized from the corresponding diol and 2-chloro-2-oxo-1,3,2-dioxaphospholane in the presence of THF. Then, five novel phosphorylcholines containing hydroxyl group were prepared by the corresponding phospholane and anhydrous trimethylamine in the presence of acetonitrile. Their structures were characterized by FTIR, 1H NMR and elemental analysis.展开更多
为有效提高医药中间体对映纯1,3-氧杂硫杂环戊烷(P_(R))的产率,本研究对动态动力学拆分,制备P_(R),并建立其动力学模型。采用一锅法合成对映纯((R)-5乙酰氧基-1,3-氧杂噻喃-2-基)乙基苯甲酸酯(P_(R)),其中,催化剂为固定化丝孢酵母脂肪酶...为有效提高医药中间体对映纯1,3-氧杂硫杂环戊烷(P_(R))的产率,本研究对动态动力学拆分,制备P_(R),并建立其动力学模型。采用一锅法合成对映纯((R)-5乙酰氧基-1,3-氧杂噻喃-2-基)乙基苯甲酸酯(P_(R)),其中,催化剂为固定化丝孢酵母脂肪酶(Trichosporonlaibachii CBS 5791),底物为2-(苯基甲氧基)乙醛(A),1,4-二硫-2,5-二醇(B)和乙酸苯酯(D)。研究结果表明,其转化率可以达到99.6%,产率为97.3%,对映体过量百分率(enantiomeric excess,ee%)为96.5%,所建立的反应体系动力学模型,很好地拟合了实验数据,表明可逆半硫代乙缩醛转化反应动力学遵从幂律方程,而酶催化内酯化反应为带产物抑制的序列机制。该研究可高效合成P_(R),最大限度地提高了生产效率。展开更多
文摘In order to construct the zwitterionic structure of phosphorylcholine onto the surface of biomaterials, five novel phospholanes containing hydroxyl group were synthesized from the corresponding diol and 2-chloro-2-oxo-1,3,2-dioxaphospholane in the presence of THF. Then, five novel phosphorylcholines containing hydroxyl group were prepared by the corresponding phospholane and anhydrous trimethylamine in the presence of acetonitrile. Their structures were characterized by FTIR, 1H NMR and elemental analysis.
文摘为有效提高医药中间体对映纯1,3-氧杂硫杂环戊烷(P_(R))的产率,本研究对动态动力学拆分,制备P_(R),并建立其动力学模型。采用一锅法合成对映纯((R)-5乙酰氧基-1,3-氧杂噻喃-2-基)乙基苯甲酸酯(P_(R)),其中,催化剂为固定化丝孢酵母脂肪酶(Trichosporonlaibachii CBS 5791),底物为2-(苯基甲氧基)乙醛(A),1,4-二硫-2,5-二醇(B)和乙酸苯酯(D)。研究结果表明,其转化率可以达到99.6%,产率为97.3%,对映体过量百分率(enantiomeric excess,ee%)为96.5%,所建立的反应体系动力学模型,很好地拟合了实验数据,表明可逆半硫代乙缩醛转化反应动力学遵从幂律方程,而酶催化内酯化反应为带产物抑制的序列机制。该研究可高效合成P_(R),最大限度地提高了生产效率。
