Kore Anilkumar R, Parmar Gaurang
Ambion, Inc., Bioorganic Chemistry Division, 2130 Woodward St., Austin, TX 78744, USA.
Nucleosides Nucleotides Nucleic Acids. 2006 Mar;25(3):337-40. doi: 10.1080/15257770500544552.
We report an industrial scale facile synthesis of 7-methyl guanosine 5'-diphosphate, which plays an important role in synthesis of various mRNA cap analogs. An efficient and selective methylation at position 7 of guanosine 5'-diphosphate was achieved by dissolving guanosine 5'-diphosphate in water and drops wise addition of dimethyl sulfate over a period of 1 h at room temperature. The reaction was completed within 2 h and resulted in more than a 96% yield. The desired product, 7-methyl GDP was purified by using BPG column on AKTA Purifier 100. Certainly, this method has advantages over the known methylation method, in terms of yield, economy, safety, and environmental concerns.
我们报道了一种工业规模的7-甲基鸟苷5'-二磷酸的简便合成方法，该化合物在各种mRNA帽类似物的合成中起着重要作用。通过将鸟苷5'-二磷酸溶解于水中，并在室温下于1小时内逐滴加入硫酸二甲酯，实现了鸟苷5'-二磷酸7位的高效选择性甲基化。反应在2小时内完成，产率超过96%。使用AKTA Purifier 100上的BPG柱对所需产物7-甲基GDP进行了纯化。当然，就产率、经济性、安全性和环境问题而言，该方法比已知的甲基化方法具有优势。
