N-Benzyloxycarbonyl-L-Isoleucine Methyl Ester置于盐酸,氢气,溶剂黄146体系中,用 水 用作溶剂,化学反应生成L-异亮氨酸甲酯盐酸盐 参考文献:Hydantoin-Free Synthesis Of Peptide Ester Isocyanates,Isothiocyanates,And Dipeptidyl Ureas: The Application Of Zinc Dust In A Carbonylation Procedure Without Base 标题:Hydantoin-Free Synthesis Of Peptide Ester Isocyanates,Isothiocyanates,And Dipeptidyl Ureas: The Application Of Zinc Dust In A Carbonylation Procedure Without Base 摘要:在使用活性锌粉作为非碱性hcl清除剂的情况下,描述了无需使用海因(hydantoin)的肽酯异氰酸酯自由合成方法,即非schotten-Baumann条件.此外,在将氨基酸和肽酰胺转化为异氰酸酯的过程中,该方法不会产生n-酰化产物. Doi:10.1055/s-0030-1260216
专利号:US-12351573-B2 优先权日:2019-05-09 标 题:Compounds for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; CHENG KAI FAN 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.
专利号:US-10266503-B1 优先权日:2016-05-24 标 题 :Sulfoxide ligand metal catalyzed oxidation of olefins 发明人:WHITE M CHRISTINA; AMMANN STEPHEN E; LIU WEI; MA RULIN 权利人:UNIV ILLINOIS 摘要:The enantioselective synthesis of isochroman motifs has been accomplished via Pd(II)-catalyzed allylic C—H oxidation from terminal olefin precursors. Critical to the success of this goal was the development and utilization of a novel chiral aryl sulfoxide-oxazoline (ArSOX) ligand. The allylic C—H oxidation reaction proceeds with the broadest scope and highest levels asymmetric induction reported to date (avg. 92% ee, 13 examples ≥90% ee). Additionally, C(sp 3 )-N fragment coupling reaction between abundant terminal olefins and N-triflyl protected aliphatic and aromatic amines via Pd(II)/sulfoxide (SOX) catalyzed intermolecular allylic C—H amination is disclosed. A range of 52 allylic amines are furnished in good yields (avg. 76%) and excellent regio- and stereoselectivity (avg. >20:1 linear:branched, >20:1 E:Z). For the first time, a variety of singly activated aromatic and aliphatic nitrogen nucleophiles, including ones with stereochemical elements, can be used in fragment coupling stiochiometries for intermolecular C—H amination reactions.
专利号:US-6495693-B2 优先权日:1996-11-22 标题:N-(aryl/heteroaryl) amino acid derivatives, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:AUDIA JAMES E; FOLMER BEVERLY K; JOHN VARGHESE; LATIMER LEE H; NISSEN JEFFREY S; PORTER WARREN J; THORSETT EUGENE D; WU JING 权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit beta-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits beta-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-2022372022-A1 优先权日:2019-05-09 标 题:Compounds for use in synthesis of peptidomimetics
专利号:US-10919882-B2 优先权日:2019-05-09 标题:Compounds for use in synthesis of peptidomimetics
专利号:US-3891692-A 优先权日:1972-05-03 标题:N-(cyclopropylalkoxycarbonyl)amino acids 发明人:VEBER DANIEL F; BRADY STEPHEN F 权利人:MERCK & CO INC 摘要:Novel N-protected- Alpha -amino acid compounds are disclosed in which the amino functionality is protected by a cyclopropylmethoxycarbonyl or 1-cyclopropyl-ethoxycarbonyl. Processes for the synthesis of amino acids containing these protecting groups and the use of these novel amino acid compounds in the preparation of peptides are also disclosed.
[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):1793-1144. [参考文献]: I B Rozenval'D, Et Al. [参考文献]: Tsitologiia. 1990;32(3):220-6. [参考文献]: Ken-Ichi Kurotani, Et Al. Elevated Levels Of Cyp94 Family Gene Expression Alleviate The Jasmonate Response And Enhance Salt Tolerance In Rice. Plant Cell Physiol. 2015 Apr;56(4):779-89. [参考文献]: S C Alfieri, Et Al. Destruction Of Leishmania Mexicana Amazonensis Amastigotes By Leucine Methyl Ester: Protection By Other Amino Acid Esters. Parasitology. 1987 Aug:95 ( Pt 1):31-41. [参考文献]: Walter S Leal, Et Al. Sex Pheromone Of The Scarab Beetle Phyllophaga Elenans And Some Intriguing Minor Components. J Chem Ecol. 2003 Jan;29(1):15-25.
合成参考文献
参考文献:10.1038/nchembio.132 摘要:Van Zeebroeck G, Bonini BM, Versele M, Thevelein JM. Transport and signaling via the amino acid binding site of the yeast Gap1 amino acid transceptor. Nat Chem Biol. 2009 Jan;5(1):45–52. doi: 10.1038/nchembio.132.