CAS: 64263-81-6; Boc-N-Me-Tyr(Bzl)-Oh

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2130-96-3 71989-40-7 63769-58-4

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CAS号2130-96-3 B°C-O-苄基-L-酪氨酸 | CAS号74-88-4 碘甲烷 | CAS号63769-58-4 B°C-O-苄基-D-酪氨酸 | CAS号82038-34-4 b°C-N-甲基-l-酪氨酸

Methyl (2S)-2-[methyl-[(2-Methylpropan-2-yl)Oxycarbonyl]Amino]-3-(4-Phenylmethoxyphenyl)Propanoate置于柠檬酸体系中,用 水 作为反应溶剂,以453 Mg的收率获得产物boc-N-甲基-O-苄基-L-酪氨酸
参考文献:Development Of Novel Monoamine Oxidase-B (Mao-B) Inhibitors With Reduced Blood-brain Barrier Permeability For The Potential Management Of Noncentral Nervous System (Cns) Diseases
标题:Development Of Novel Monoamine Oxidase-B (Mao-B) Inhibitors With Reduced Blood-brain Barrier Permeability For The Potential Management Of Noncentral Nervous System (Cns) Diseases
摘要:Studies Indicate That Mao-B Is Induced In Peripheral Inflammatory Diseases. To Target Peripheral Tissues Using Mao-B Inhibitors That Do Not Permeate The Blood Brain Barrier (Bbb) The Mao-B-Selective Inhibitor Deprenyl Was Remodeled By Replacing The Terminal Acetylene With A Co2H Function,And Incorporating A Para-och2Ar Motif (Compounds 10A-S). Further,In Compound 32 The C-2 Side Chain Corresponded To Ch2Cn. In Vitro,10C,10J,10K,And 32 Were Identified As Potent Reversible Mao-B Inhibitors,And All Four Compounds Were More Stable Than Deprenyl In Plasma,Liver Microsomal,And Hepatocyte Stability Assays. In Vivo,They Demonstrated Greater Plasma Bioavailability. Assessment Of In Vitro Bbb Permeability Showed That Compound 10K Is A P-Glycoprotein (P-Gp) Substrate And 10J Displayed Mild Interaction. Importantly,Compounds 10C,10J,10K,And 32 Displayed Significantly Reduced Bbb Permeability After Intravenous,Subcutaneous,And Oral Administration. These Polar Mao-B Inhibitors Are Pertinent Leads For Evaluation Of Efficacy In Noncentral Nervous System (Cns) Inflammatory Disease Models.
DOI:10.1021/acs.Jmedchem.7B01588