Diethyl (N-Acetylamino)[(1-Naphthyl)Methyl]Malonate置于盐酸,Sodium Hydroxide体系中,用 乙醇 作为反应溶剂,化学反应 8.17H,反应生成 3-(1-萘基)-L-丙氨酸 参考文献:Synthesis And Biological Activities Of Cholecystokinin Analogues Substituted In Position 30 By 3-(1-Naphthyl)-L-Alanine [nal(1)] Or 3-(2-Naphthyl)-L-Alanine [nal(2)] 标题:Synthesis And Biological Activities Of Cholecystokinin Analogues Substituted In Position 30 By 3-(1-Naphthyl)-L-Alanine [nal(1)] Or 3-(2-Naphthyl)-L-Alanine [nal(2)] 摘要:Acetyl Derivatives Of Ethyl Esters Of 3-(1-Naphthyl)-D,L-Alanine And 3-(2-Naphthyl)-D,L-Alanine Were Synthesized Through A Malonic Condensation. Resolution Of These Derivatives By Subtilisin Carlsberg Followed By Acid Hydrolysis Afforded The 2 Optical Isomers Of 3-(1-Naphthyl)-Alanine [nal(1)] And 3-(2-Naphthyl)-Alanine [nal(2)]. The L Enantiomers Of These Amino Acids Were Incorporated Into The Sequence Of Cholecystokinin In Place Of The Tryptophan In Position 30. The Cholecystokinin Analogues Thus Obtained Behaved As Full Agonists,With Reduced Potencies On Rat Pancreatic Acini And On Guinea Pig Brain Membranes,By About One Order Of Magnitude For The Nal(2) Derivative And By 2 Orders Of Magnitude For The Nal(1) Derivative,As Compared To The Potent Parent Compound Boc-Tyr(So3H)-Nle-Gly-Trp-Nle-Asp-Phe-Nh2. DOI:10.1016/0223-5234(91)90056-S
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-2024209029-A1 优先权日:2021-04-21 标题:Adiponectin glycopeptides and compositions and methods of use thereof 发明人:WANG YU; LI XUECHEN; XU AIMIN; WU HONGXIANG; ZHANG YIWEI; LI YUANXIN 权利人:UNIV HONG KONG 摘要:An improved method for the chemical synthesis of glycosylated peptides has been developed. The method uses stereoselective glycan synthesis and chemical peptide ligation to produce glycopeptides at lower-cost and with higher efficiency/yield compared to conventional methods. In particular, a method for the large-scale, chemical synthesis of hydroxylated amino acid building blocks and glycosylated amino acids suitable for solid phase peptide synthesis (SPPS) are disclosed. SPPS-based methods using the glycosylated amino acids to chemically synthesize adiponectin-like peptides are also described. In vivo studies show that the adiponectin mimicking glycopeptides exhibit significant anticancer, anti-obesity and insulin sensitizing effects. Pharmaceutical compositions of the synthetic glycopeptides and methods of use thereof in treating diseases associated with deficient adiponectin are also described.
专利号:US-2024218014-A1 优先权日:2022-11-21 标 题:Synthesis of a cyclic peptide 发明人:BAUR PIUS BRUNO; CLEATOR EDWARD; DENIAU GILDAS; EISELE FRANK; FLÖGEL OLIVER; HUSTE ANJA; KEHL MARCEL ROMAN; LÖWENECK MARKUS; SILVA ROLANDO RAVELO; VORBERG RAFFAEL 权利人:JANSSEN PHARMACEUTICA NV 摘要:Processes for performing peptide synthesis, particularly for cyclic peptide synthesis are generally described. Reaction intermediates of the peptide synthesis are also described.
专利号:WO-9717367-A1 优先权日:1995-11-03 标 题 :Method of grf peptides synthesis 发明人:IBEA MICHEL; BRAZEAU PAUL 权利人:THERATECHNOLOGIES INC 摘要:The present invention relates to a high yield manufacturing process of (Gly or Ala)?15 or 32¿ GRF containing peptide, resulting in GRF peptides synthesis at a yield averaging 65 to 68 %. The method comprises the steps of: a) synthesis of a 14 to 15 residues of the fully protected GRF peptide acidic segments (S¿1?)-OH and (S2)-OH from sasrin resin, using sequential Fmoc chemistry; b) synthesis of a 12 to 15 residues of the side chain protected GRF peptide amide segments (S3)-NH-, (S4)-NH-, and/or (S5)-NH- on solid phase using any TFA sensitive resin; and c) one or two coupling steps of the synthesized GRF peptide segments of steps a) and b) on solid phase.
专利号:US-2024400608-A1 优先权日:2021-09-03 标题:Synthesis of bicycle toxin conjugates, and intermediates thereof 发明人:WITTY DAVID; LIMB DARREN; MIN BYOUNG JOON; HE LIWEN; SANDERS WILLIAM J; NNANABU ERNEST OBINNA 权利人:BRICYCLETX LTD 摘要:The present invention relates to Bicycle toxin conjugates, methods for preparation, and methods of use for treating cancer.
专利号:US-2023037284-A9 优先权日:2018-11-30 标题:Combination therapy of peptidomimetic macrocycles 发明人:GUERLAVAIS VINCENT; ANNIS DAVID ALLEN 权利人:AILERON THERAPEUTICS INC 摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.
[参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1034.
合成参考文献
摘要:Nguyen, B. N.; Hii, K. K.; Szymański, W.; Janssen, D. B., Science of Synthesis: Stereoselective Synthesis, (2011) 1, 643. 参考文献:10.1007/bf01388169 摘要:Miyazawa T. Enzymatic resolution of amino acids via ester hydrolysis. Amino Acids. 1999;16(3-4):191–213. doi: 10.1007/bf01388169.