📜Dl-苯丙氨酸置于氯化亚砜体系中,用 甲醇 作为反应溶剂,以93.61%的收率获得产物dl-苯基丙氨酸甲酯盐酸盐 参考文献:Design And Bio-Evaluation Of Indole Derivatives As Potent Kv1.5 Inhibitors 标题:Design And Bio-Evaluation Of Indole Derivatives As Potent Kv1.5 Inhibitors 摘要:Atrial Fibrillation (Af) Is One Of The Common Arrhythmias That Threaten Human Health. Kv1.5 Potassium Channel Is Reported As An Efficacious And Safe Target For The Treatment Of Af. In This Paper,We Designed And Synthesized Three Series Of Compounds Through Modifying The Lead Compound Rh01617 That Was Screened Out By The Pharmacophore Model We Reported Earlier. All Of The Compounds Were Evaluated By The Whole-Patch Lamp Technology And Most Of Them Possessed Potent Inhibitory Activities Against Kv1.5. Compounds Iiii And Iiil Were Evaluated For The Target Selectivity As Well As The Pharmacodynamic Effects In An Isolated Rat Model. Due To The Promising Pharmacological Behavior,Compound Iiil Deserves Further Pharmacodynamic And Pharmacokinetic Evaluations. (C) 2013 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Bmc.2013.08.041
专利号:US-10829792-B2 优先权日:2017-03-21 标 题 :Biocatalytic synthesis of strained carbocycles 发明人:CHEN KAI; HUANG XIONGYI; KAN S B JENNIFER 权利人:CALIFORNIA INST OF TECHN 摘要:Provided herein are methods for producing products containing strained carbocycles, such as cyclopropene moieties and/or bicyclobutane moieties. The methods include combining an alkyne and a carbene precursor in the presence of a heme protein, e.g., a cytochrome P450, under conditions sufficient to form the strained carbocycle. Reaction mixtures for producing strained carbocycles are also described, as well as whole-cell catalysts comprising heme proteins and variants thereof for forming cyclopropenes, bicyclobutanes, and related products.
专利号:US-6077962-A 优先权日:1998-12-24 标题 :N-3, 3-dimethylbutyl-L-aspartic acid and esters thereof, the process of preparing the same, and the process for preparing N-(N-(3,3-dimethylbutyl) -α L-aspartyl)-L- phenylalanine 1-methyl ester therefrom 发明人:PRAKASH INDRA; CHAPEAU MARIE-CHRISTINE D 权利人:NUTRASWEET CO 摘要:This invention relates to the chemical synthesis of N-[N-(3,3-dimethylbutyl)-L-α-aspartyl]-L-phenylalanine 1-methyl ester using peptide coupling methods. The coupling reaction is conducted by condensation of an activated derivative of novel N-neohexyl-L-aspartic acid with L-phenylalanine or L-phenylalanine methyl ester or by enzymatic coupling of N-neohexyl-L-aspartic acid with L-phenylalanine or L-phenylalanine methyl ester. This invention also relates to novel N-(3,3-dimethylbutyl)-L-aspartic acid, derivatives thereof and the preparation thereof. The activated derivative of N-neohexyl-L-aspartic acid may be an anhydride, mixed anhydride, active ester or an intermediate activated derivative thereof.
专利号:US-2009018343-A1 优先权日:2005-03-16 标题 :Fluorous Oxazolidinone Chiral Auxiliary Compounds and Methods of Manufacture 发明人:HULTIN PHILIP GREGORY; HEIN JASON ELLIS 权利人:UNIV MANITOBA 摘要:The present invention relates generally to perfluoroalkyl chiral auxiliary compounds and methods of manufacture. These compounds have the functionality to effectively support the synthesis of chiral compounds in single reactions, high-throughput parallel reactions, or combinatorial reactions The invention relates to two oxazolidinone chiral auxiliaries (1) and (2): wherein R f is a perfluoroalkyl group having the general formula (CH 2 ) x —C y F 2y+1 where x=1-5 and y=4-10 and wherein B is an unfunctionalized aryl, alkyl or arylalkyl group in a preferred embodiment, x=2 and y=6 and B is derived from unfunctionalized amino acids The amino acids may be from either the D- or L-series, and are preferably enantiomerically pure or in very high enantiomeric excess in either configuration.
专利号:US-2024182642-A1 优先权日:2022-11-23 标 题:Green synthesis of amino acid based poly(ester urea)s 发明人:OLSEN BRADLEY DAVID; FRANSEN KATHARINA 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Disclosed are methods of synthesizing poly(ester urea)s.
专利号:CN-104774891-A 优先权日:2015-01-15 标题:A kind of technique of enzymatic efficient synthesis of benzyloxycarbonyl aspartame
专利号:CN-104774891-B 优先权日:2015-01-15 标 题:A kind of technique of enzymatic efficient synthesis of benzyloxycarbonyl aspartame
参考文献:10.1080/14756366.2022.2070909 摘要:Kaur S, Nieto NS, McDonald P, Beck JR, Honzatko RB, Roy A, Nelson SW. Discovery of small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase. Journal of Enzyme Inhibition and Medicinal Chemistry. 2022 May 05;37(1):1320–6. doi: 10.1080/14756366.2022.2070909.