Okada Yohei, Hosoya Shoichi, Suzuki Hidenobu, Chiba Kazuhiro
Department of Applied Biological Chemistry, Tokyo University of Agriculture and Technology , 3-5-8 Saiwai-cho, Fuchu, Tokyo 183-8509, Japan.
Org Lett. 2014 Dec 19;16(24):6448-51. doi: 10.1021/ol5032798. Epub 2014 Dec 10.
A highly aggregating elastin peptide was prepared efficiently using a high pressure-liquid phase synthesis approach assisted by a soluble tag strategy. Two standard syringes were connected to each other to construct a reactor. This simple reactor was used to apply high pressure to the highly viscous reaction mixture thereby maintaining its fluidity. The reactions were completely inhibited due to aggregation when conducted in a standard flask reactor, whereas our high pressure approach accelerated the couplings to realize complete conversion within 5-7 min. All steps were conducted at 0.10 M concentration, affording grams of the desired product.
采用可溶性标签策略辅助的高压液相合成方法，高效制备了一种高度聚集的弹性蛋白肽。将两个标准注射器相互连接以构建一个反应器。这个简单的反应器用于对高粘性反应混合物施加高压，从而保持其流动性。在标准烧瓶反应器中进行反应时，由于聚集反应完全受到抑制，而我们的高压方法加速了偶联反应，在5 - 7分钟内实现了完全转化。所有步骤均在0.10 M浓度下进行，得到了克级的所需产物。
