N-苄氧羰基-L-色氨酸置于10Percent Pd/c N-甲基吗啉,盐酸,氢气,氯甲酸异丁酯体系中,用 乙二醇二甲醚,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 24.0H,反应生成 L-色氨酰胺盐酸盐 参考文献:New Active Series Of Growth Hormone Secretagogues 标题:New Active Series Of Growth Hormone Secretagogues 摘要:New Growth Hormone Secretagogue (Ghs) Analogues Were Synthesized And Evaluated For Growth Hormone Releasing Activity. This Series Derived From Ep-51389 Is Based On A Gem-Diamino Structure. Compounds That Exhibited Higher In Vivo Gh-Releasing Potency Than Hexarelin In Rat (Subcutaneous Administration) Were Then Tested Per Os In Beagle Dogs And For Their Binding Affinity To Human Pituitary Ghs Receptors And To Hghs-R 1A. Compound 7 (Jmv 1843,H-Aib-(D)-Trp-(D)-Gtrp-Formyl) Showed High Potency In These Tests And Was Selected For Clinical Studies.(1) DOI:10.1021/jm020985Q
[参考文献]: Cássia Alessandra Marquezin, Et Al. Tryptophan As A Probe For Acid-Base Equilibria In Peptides. Biopolymers. 2003;71(5):569-76. [参考文献]: D Andrews, Et Al. Tryptophanamide Formation By Escherichia Coli Tryptophanyl-Trna Synthetase. Eur J Biochem. 1985 Jan 2;146(1):201-9. [参考文献]: D Prschke, Et Al. Stability Decrease Of Rna Double Helices By Phenylalanine-, Tyrosine- And Tryptophane-Amides. Analysis In Terms Of Site Binding And Relation To Melting Proteins. Nucleic Acids Res. 1982 Oct 11;10(19):6163-76. [参考文献]: Krishanu Ray, Et Al. Metal-Enhanced Intrinsic Fluorescence Of Proteins On Silver Nanostructured Surfaces Towards Label-Free Detection. J Phys Chem C Nanomater Interfaces. 2008;112(46):17957-17963. [参考文献]: Pedro L Muio, Et Al. Solvent Effects On The Fluorescence Quenching Of Tryptophan By Amides Via Electron Transfer. Experimental And Computational Studies. J Phys Chem B. 2009 Mar 5;113(9):2572-7.
合成参考文献
参考文献:10.1107/s0108768100013975 摘要:In Y, Fujii M, Sasada Y, Ishida T. Structural studies on C-amidated amino acids and peptides: structures of hydrochloride salts of C-amidated Ile, Val, Thr, Ser, Met, Trp, Gln and Arg, and comparison with their C-unamidated counterparts. Acta Crystallogr B. 2001 Feb;57(Pt 1):72–81. doi: 10.1107/s0108768100013975.