Institute of Petrochemistry and Catalysis, Russian Academy of Sciences, 141 Prospekt Oktyabrya, 450075, Ufa, Russian Federation.
Chem Commun (Camb). 2013 Sep 28;49(75):8401-3. doi: 10.1039/c3cc44926b.
An original, effective approach to the synthesis of natural and synthetic 5Z,9Z-dienoic acids in high yields (61-67%) and with high selectivity (>98%) was developed. The approach is based on the use of the new intermolecular catalytic cross cyclomagnesiation of terminal aliphatic and oxygenated 1,2-dienes upon treatment with Grignard reagents in the presence of the Cp2TiCl2 catalyst. High activity of (5Z,9Z)-5,9-eicosadienoic acid as a human topoisomerase I inhibitor at concentrations above 0.1 μM was elucidated.
开发了一种新颖、有效的方法，可高产（61-67%）且高选择性（>98%）地合成天然和合成的 5Z,9Z-二烯酸。该方法基于在 Cp2TiCl2 催化剂存在下，用格氏试剂处理时，新的末端脂肪族和含氧 1,2-二烯的分子间催化交叉环镁化作用。研究了（5Z,9Z）-5,9-二十碳二烯酸在 0.1μM 以上浓度时作为人拓扑异构酶 I 抑制剂的高活性。
