Boc和Fmoc保护氨基酸与M树脂和王氏树脂结合率的比较

M树脂与Boc保护的亮氨酸、甘氨酸或苯丙氨酸的铯盐成酯反应摩尔比1:1.2,时间31h,其产物用重量法和水杨醛法测得的结合率均值分别为87.3%、89.1%和89.6%。王氏树脂与Fmoc保护的亮氨酸、甘氨酸或苯丙氨酸反应48h,树脂:Fmoc氨基酸:DCC:DMAP摩尔比为1:3:4:1,其产物结合率的均值分别为44.2%、30.4%和56.2%。结果表明,前者产物结合率高于后者。另外,重量法与水杨醛法测得的结合率相差不超过2.7%,但重量法更方便,易行。

A comparison between the yield of the attachment of Boc-AA-O^-Cs^+ to merrifield resin and of Fmoc-AA-OH to Wang resin

The yields of the attachment of Boc - Lue - O- Cs , Boc - Gly - O- Cs or Boc - Phe - O- Cs (1.2 eqv. ) to Merrifield resin(1.0 eqv.) for 31 hours is 87.3% , 89.1% or 89.6% (the mean values of those detected by weight and by these measured the free amino group, respectively) . The yields of the anchoring of Fmoc - Lue - OH, Fmoc-Gly- OH or Fmoc - Phe - OH(3.0 eqv. ) to Wang resin(l .0 eqv.) for 48 hours is 44.2% , 30.4% or 56.2% (the mean values of those detected by weight and those measured by the free amino group, respectively). The results show that the combination ratio of Boc - strategy is at least 33 .4% higher than that of the Fmoc - strategy. In addition, difference in the combination ratios between those determined by weight and the those by the free amino group is below 2.7% , but weight method is more convenient and feasible.