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📜(+/-)-3-(3,4-Dihydroxyphenyl)-2-Methyl-Dl-Alanine置于alcalase,水体系中,用 叔丁醇 作为反应溶剂,化学反应 2.5H,反应生成 3-羟基-D-酪氨酸
参考文献:Chemo-Enzymatic Synthesis Of Optically Active Amino Acids And Peptides
标题:Chemo-Enzymatic Synthesis Of Optically Active Amino Acids And Peptides
摘要:Abstractthe Industrial Alkaline Protease,Alcalase,Is Stable And Active In A High Concentration Of Organic Solvents And Useful As A Biocatalyst For (I) Diastereoselective Hydrolysis Of Peptide Esters And Preparation Of Racemization‐free Peptides; (II) Selective Incorporation Of Esters Of D‐amino Acid Into Peptides In T‐butanol Via A Selective Hydrolysis Of Esters Of D,L‐amino Acid,Followed By Using The Unhydrolyzed D‐esters As A Nucleophile In A Kinetically Controlled Peptide Bond Formation; (Iii) Resolution Of Esters Of Amino Acid In 95% T‐butanol/5% Water,Followed By Saponification Of The Unreacted Esters To Offer Both Enantiomers With High Yield And Optical Purity; (Iv) Completely Resolve Amino‐acid Esters With High Yield And Optical Purity Via In Situ Racemization Of The Unreacted Antipode Catalyzed By Pyridoxal 5‐phosphate; (V) Cryobioorganic Synthesis Of Peptides With Increased Yields 15%-40% Of Peptide Bond Formation By Reaction At 5 oc Instead Of 25-30 oc Of A Kinetically Controlled Enzymatic Reaction In Alcohols.
DOI:10.1002/jccs.199900046

专利信息

专利号:WO-9312076-A1
优先权日:1991-12-13
标题:Reagents for automated synthesis of peptide analogs
发明人：WEBB THOMAS ROY
权利人:CORVAS INT INC
摘要:Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.

专利号:US-5283293-A
优先权日:1990-12-14
标 题:Reagents for automated synthesis of peptide analogs
发明人：WEBB THOMAS R
权利人:CORVAS INC
摘要:Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.

专利号:US-5367072-A
优先权日:1990-12-14
标 题 :Reagents for automated synthesis of peptide analogs
发明人：WEBB THOMAS R
权利人:CORVAS INT INC
摘要:Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.

专利号:US-2006030625-A1
优先权日:2004-08-06
标 题 :Dietary neurotransmitter precursors for balanced synthesis of neurotransmitters
发明人：HART CHERYLE RAM; GROSSMAN RONALD S; RAM HERBERT
权利人:HART CHERYLE RAM; GROSSMAN RONALD S; RAM HERBERT
摘要:Dietary supplements for treating a neurotransmitter deficiency include one or more precursors of the deficient neurotransmitter and a cofactor for activating in vivo enzymatic synthesis of the deficient neurotransmitter. The dietary supplements can also include an appropriate neurotransmitter, such as an amino acid. When administered through the oral mucosa, increases in levels of the deficient neurotransmitters and relief from deficiency symptoms are obtained.

专利号:US-9475837-B2
优先权日:2011-12-23
标题 :Process for the synthesis of therapeutic peptides
发明人：HURLEY FIONN; WEGNER KATARZYNA; FOLEY PATRICK
权利人:IPSEN MFG IRELAND LTD
摘要:The present invention relates to a process for the large-scale synthesis of therapeutic peptides using a Sieber Amide resin, which comprises solid-phase Fmoc-chemistry.

专利号:US-2004053355-A1
优先权日:2000-05-26
标题:Modular approach to on-line synthesis, drug discovery and biochemical transformations using immobilized enzyme reactors
发明人：WAINER IRVING; MARKOGLOU NEKTARIA
摘要:A coupled system using extremely different enzymes with incompatible cofactors and reaction conditions has been constructed using standard liquid chromatographic formats and open tubular formats. One of the significant aspects of the present invention lies in the development of the liquid chromatographic on-line enzyme cascade. This has been illustrated by the biosynthetic pathway involving dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase which encompass the synthesis of the key neurotransmitters, norepinephrine and epinephrine. The results demonstrate for the first time the immobilization of dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase. The IMERs are active and can be used in a liquid chromatographic format for qualitative and quantitative determinations. The IMER-HPLC system can be used to carry out standard Michaelis-Menten enzyme kinetic studies and to quantitatively determine enzyme kinetic constants, identify specific enzyme inhibitors, provide information regarding the mode of inhibition and the inhibitor constants (K i ). A second significant aspect of the present invention lies in the ability of the immobilized enzyme reactors to be used independently or as a combination, thus providing a unique opportunity to explore the interrelationships between these enzymes, to investigate the source of diseases and to design new drug entities for identified clinical syndromes.