Haug Bengt Erik, Rich Daniel H
School of Pharmacy, University of Wisconsin-Madison, Madison, Wisconsin 53706, USA.
Org Lett. 2004 Dec 9;6(25):4783-6. doi: 10.1021/ol047879y.
[structure: see text] The protected Gln-Phe hydroxyethylene dipeptide isostere 1 was synthesized as a precursor for preparation of potential inhibitors of Botulinum neurotoxin B metalloprotease. The method allows for the synthesis of additional hydroxyethylene dipeptide isosteres such as 2 with functionalized P1 side chains. The isosteres prepared were coupled with a dipeptide to produce protected pseudotetrapeptide derivatives.
[结构：见文本] 受保护的谷氨酰胺-苯丙氨酸羟乙烯二肽类似物1被合成为制备肉毒杆菌神经毒素B金属蛋白酶潜在抑制剂的前体。该方法允许合成带有功能化P1侧链的其他羟乙烯二肽类似物，如2。所制备的类似物与二肽偶联以产生受保护的假四肽衍生物。
