COMPARATIVE-STUDIES OF THE COUPLING OF N-METHYLATED, STERICALLY HINDERED AMINO-ACIDS DURING SOLID-PHASE PEPTIDE-SYNTHESIS
COMPARATIVE-STUDIES OF THE COUPLING OF N-METHYLATED, STERICALLY HINDERED AMINO-ACIDS DURING SOLID-PHASE PEPTIDE-SYNTHESIS
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DOI：
10.1016/0040-4039(94)88054-9
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发表时间：
1994-08-15
影响因子：
1.8
通讯作者：
RICH, DH
中科院分区：
文献类型：
--
作者：
ANGELL, YM;GARCIAECHEVERRIA, C;RICH, DH
在固相肽合成(SPPS)条件下，比较了不同偶联剂对N-甲基化、空间位阻氨基酸的有效偶联作用。偶联剂1-羟基-7-氮杂苯并三氮唑(HOAT)及其铀盐衍生物(HATU)均能产生定量偶联，得到了较好的结果。报道了这些试剂在合成环孢素中发现的2-7序列中的应用。
Comparison of different coupling reagents for effective coupling of N-methylated, sterically hindered amino acids under solid-phase peptide synthesis (SPPS) conditions is described. Superior results were obtained with the coupling additive 1-hydroxy-7-azabenzotriazole (HOAt), as well as its uronium salt derivative (HATU), which both produced quantitative couplings. Application of these regents to the synthesis of the 2-7 sequence found in cyclosporin is reported.