Enantioselective syntheses of alpha-Fmoc-Pbf-[2-(13)C]-L-arginine and Fmoc-[1,3-(13)C2]-L-proline and Incorporation into the neurotensin receptor 1 ligand, NT(8-13).
Enantioselective syntheses of alpha-Fmoc-Pbf-[2-(13)C]-L-arginine and Fmoc-[1,3-(13)C2]-L-proline and Incorporation into the neurotensin receptor 1 ligand, NT(8-13).
复制标题
α-Fmoc-Pbf-[2-(13)C]-L-精氨酸和 Fmoc-[1,3-(13)C2]-L-脯氨酸的对映选择性合成并掺入神经降压素受体 1 配体 NT(8
DOI：
10.1021/jo9014497
复制
发表时间：
2009
期刊：
影响因子：
--
通讯作者：
Song C
中科院分区：
文献类型：
--
作者：
Song C
描述了由市售前体[2 - 13 C]溴乙酸和[13 C]氰化钾对映选择性合成选择性标记的正交保护的[2 - 13 C]-L-精氨酸和[1，3 - 13 C 2]-L-脯氨酸。有趣的是，在室温下，α-Fmoc-Pbf-[2- 13 C]-l-精氨酸的13 C NMR谱中，C-2的增强信号非常宽。使用这两种Fmoc标记的氨基酸，通过手动Fmoc-SPSS制备[2- 13 C]-Arg 9和[1，3 - 13 C2]-Pro 10标记的配体（NT 8 −13）。
Enantioselective syntheses of selectively labeled, orthogonally protected [2-13C]-l-arginine and [1,3-13C2]-l-proline are described from the commercially available precursors [2-13C]bromoacetic acid and potassium [13C]cyanide. Interestingly the enhanced signal assigned to C-2 in the13C NMR spectrum of α-Fmoc-Pbf-[2-13C]-l-arginine was very broad at room temperature. The two Fmoc-labeled amino acids were used to prepare [2-13C]-Arg9 and [1,3-13C2]-Pro10 labeled ligand (NT8−13) by manual Fmoc-SPSS.