Stern M, Warshawksy A, Fridkin M
Int J Pept Protein Res. 1981 May;17(5):531-8. doi: 10.1111/j.1399-3011.1981.tb02025.x.
Insoluble 2-mercaptopyridine and 2-mercapto-nitrobenzene derivatives were prepared by modification of commercially available polystyrene. Applicability of these polymers as reagents for the thiolytic removal of the 2-nitrophenylsulphenyl amino-protecting group and as supports for preparation of polymeric active esters was evaluated. Polymeric 2-mercaptopyridine (PMP) was found efficient for both purposes. It was used in the stepwise synthesis of Leu-enkephalin via the polymeric reagent approach, serving as an Nps-cleaver. Polymeric esters derived from PMP and Boc-amino acids proved to be excellent acylators. Their usefulness is exemplified in the preparation of two dipeptides, which were produced rapidly and in high yields and purity.
通过对市售聚苯乙烯进行改性制备了不溶性2-巯基吡啶和2-巯基硝基苯衍生物。评估了这些聚合物作为用于硫解去除2-硝基苯硫基氨基保护基的试剂以及作为制备聚合物活性酯的载体的适用性。发现聚合物2-巯基吡啶（PMP）对这两个目的均有效。它通过聚合物试剂方法用于亮氨酸脑啡肽的逐步合成，用作Nps切割剂。由PMP和Boc-氨基酸衍生的聚合物酯被证明是优异的酰化剂。它们的实用性在两种二肽的制备中得到了体现，这两种二肽快速、高产率且高纯度地制备出来。
