CAS: 19914-38-6; (R)-2-((Tert-Butoxycarbonyl)(Methyl)Amino)Propanoic Acid

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13734-31-1 1142-20-7 15761-38-3

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N-(tert-butyloxycarbonyl) azide B°C-(R)-Ala methyl iodide tert-butyl dicarbonatedi-tert-butyl dicarbonate(S)-1-[(R)-2-(tert-Butoxycarbonyl-methyl-amino)-propionyl]-pyrrolidine-2-carboxylic acid benzyl ester 2S-[[2R-[N-(tert-butoxycarbonyl)-N-(methyl)amino]propionyl]amino]-N-[2R-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1S-(phenylmethyl)propyl]-3,3-dimethylbutanamide 20H30N2O6C20H30N2O6

二碳酸二叔丁酯置于sodium Hydride,Sodium Carbonate体系中,用 四氢呋喃,水 用作溶剂,化学反应 73.0H,反应生成Boc-N-甲基-D-丙氨酸
参考文献:Phase I Metabolites Of Mephedrone Display Biological Activity As Substrates At Monoamine Transporters
标题:Phase I Metabolites Of Mephedrone Display Biological Activity As Substrates At Monoamine Transporters
摘要:Background And Purpose4‐methyl‐n‐methylcathinone (Mephedrone) Is A Synthetic Stimulant That Acts As A Substrate‐type Releaser At Transporters For Dopamine (Dat),Noradrenaline (Net) And 5‐ht (Sert). Upon Systemic Administration,Mephedrone Is Metabolized To Several Phase I Compounds: The N‐demethylated Metabolite,4‐methylcathinone (Nor‐mephedrone); The Ring‐hydroxylated Metabolite,4‐hydroxytolylmephedrone (4‐oh‐mephedrone); And The Reduced Keto‐metabolite,Dihydromephedrone.Experimental Approachwe Used In Vitro Assays To Compare The Effects Of Mephedrone And Synthetically Prepared Metabolites On Transporter‐mediated Uptake And Release In Hek293 Cells Expressing Human Monoamine Transporters And In Rat Brain Synaptosomes. In Vivo Microdialysis Was Employed To Examine The Effects Of I.V. Metabolite Injection (1 And 3 Mg.kg−1) On Extracellular Dopamine And 5‐ht Levels In Rat Nucleus Accumbens.Key Resultsin Cells Expressing Transporters,Mephedrone And Its Metabolites Inhibited Uptake,Although Dihydromephedrone Was Weak Overall. In Cells And Synaptosomes,Nor‐mephedrone And 4‐oh‐mephedrone Served As Transportable Substrates,Inducing Release Via Monoamine Transporters. When Administered To Rats,Mephedrone And Nor‐mephedrone Produced Elevations In Extracellular Dopamine And 5‐ht,Whereas 4‐oh‐mephedrone Did Not. Mephedrone And Nor‐mephedrone,But Not 4‐oh‐mephedrone,Induced Locomotor Activity.Conclusions And Implicationsour Results Demonstrate That Phase I Metabolites Of Mephedrone Are Transporter Substrates (I.E. Releasers) At Dat,Net And Sert,But Dihydromephedrone Is Weak In This Regard. When Administered In Vivo,Nor‐mephedrone Increases Extracellular Dopamine And 5‐ht In The Brain Whereas 4‐oh‐mephedrone Does Not,Suggesting The Latter Metabolite Does Not Penetrate The Blood-brain Barrier. Future Studies Should Examine The Pharmacokinetics Of Nor‐mephedrone To Determine Its Possible Contribution To The In Vivo Effects Produced By Mephedrone.
Doi:10.1111/bph.13547