CAS: 114873-05-1; Boc-Phe(2-Me)-Oh

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80102-29-0 211637-75-1 80126-53-0

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tert-butyl dicarbonatedi-tert-butyl dicarbonate 2'-methyl-(2S)-α-phenylalanineα-tert-butyloxycarbonyl-2'-methyl-L-phenylalanyl-L-phenylalanylamideNα-tert-butyloxycarbonyl-2'-methyl-L-phenylalanyl-L-phenylalanylamide α-tert-butyloxycarbonyl-L-tyrosyl-L-prolyl-2'-methyl-L-phenylalanyl-L-phenylalanylamideNα-tert-butyloxycarbonyl-L-tyrosyl-L-prolyl-2'-methyl-L-phenylalanyl-L-phenylalanylamide α-tert-butyloxycarbonyl-2',6'-dimethyl-L-tyrosyl-L-prolyl-2'-methyl-L-phenylalanyl-L-phenylalanylamideNα-tert-butyloxycarbonyl-2',6'-dimethyl-L-tyrosyl-L-prolyl-2'-methyl-L-phenylalanyl-L-phenylalanylamide 34H48N6O7S2C34H48N6O7S2

二碳酸二叔丁酯,L-2-甲基苯丙氨酸置于三乙胺体系中,用 1,4-二氧六环,水 用作溶剂,化学反应 2.0H,以89.2%的收率获得boc-L-2-甲基苯丙氨酸
参考文献:Bifunctional [2',6'-Dimethyl-L-Tyrosine]Endomorphin-2 Analogues Substituted At Position 3 With Alkylated Phenylalanine Derivatives Yield Potent Mixed μ-Agonist/δ-Antagonist And Dual μ-Agonist/δ-Agonist Opioid Ligands
标题:Bifunctional [2',6'-Dimethyl-L-Tyrosine]Endomorphin-2 Analogues Substituted At Position 3 With Alkylated Phenylalanine Derivatives Yield Potent Mixed μ-Agonist/δ-Antagonist And Dual μ-Agonist/δ-Agonist Opioid Ligands
摘要:Endomorphin-2 (H-Tyr-Pro-Phe-Phe-Nh2) And [dmt(1)]Em-2 (Dmt = 2',6'-Dimethyl-L-Tyrosine) Analogues,Containing Alkylated Phe(3) Derivatives,2'-Monomethyl (2,2'),3',5'-And 2',6'-Dimethyl (3,3',And 4',Respectively),2',4',6'-Trimethyl (6,6'),2'-Ethyl-6'-Methyl (7,7'),And 2'-Isopropyl-6'-Methyl (8,8') Groups Or Dmt (5,5'),Had The Following Characteristics: (I) [xaa(3)]Em-2 Analogues Exhibited Improved Mu-And Delta-Opioid Receptor Affinities. The Latter,However,Were Inconsequential (K-I(Delta) = 491-3451 Nm). (II) [dmt(1),Xaa(3)]Em-2 Analogues Enhanced Mu-And Delta-Opioid Receptor Affinities (K-I(Mu) = 0.069-0.32 Nm; K-I(Delta) = 1.83-99.8 Nm) Without Kappa-Opioid Receptor Interaction. (III) There Were Elevated Mu-Bioactivity (Ic50 = 0.12-14.4 Nm) And Abolished Delta-Agonism (Ic50 > 10 Mu M In 2',3',4',5',6'),Although 4' And 6' Demonstrated A Potent Mixed Mu-Agonism/delta-Antagonism (For 4',Ic50 Mu = 0.12 And Pa(2) = 8.15; For 6',Ic50 Mu = 0.21 Nm And Pa(2) = 9.05) And 7' Was A Dual Mu-Agonist/delta-Agonist (Ic50 Mu = 0.17 Nm; Ic50 Delta = 0.51 Nm).
Doi:10.1021/jm061238M