CAS: 1078-61-1; 3-(3,4-Dihydroxyphenyl)Propionic Acid

该化合物是一种在结构上与咖啡叶酸有关的酚类化合物,其特点是两个氢氧基组和芳香环中的双联,这助长了其抗氧化性特性,该化合物通常存在于各种植物来源,以其潜在的健康惠益,包括抗炎和...

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3598-22-9 545442-98-6 621-54-5

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合成工艺路线路线简述

  • 合成目标产物 Dihydrocaffeic Acid 主要起始原料 Caffeic Acid
  • (文献来源)合成步骤主要原料 Caffeic Acid
左旋多巴置于tyrosine Transaminase体系中,化学反应生成3,4-二羟基苯基丙酸
参考文献:Unusual Isomeric Corniculatolides From Mangrove,Aegiceras Corniculatum
标题:Unusual Isomeric Corniculatolides From Mangrove,Aegiceras Corniculatum
摘要:Four New Isomeric Macrolides Of Combretastatin D-2 Congeners Named Isocorniculatolide A (1),11-O-Methylisocorniculatolide A (2),11-O-Methylcomiculatolide A (3),And 12-Hydroxy-11-O-Methylcorniculatolide A (4),And The Known Corniculatolide A (5),Arjunolic Acid,And Maslinic Acid Were Isolated From The Chcl3 Extract Of The Bark Of Aegiceras Corniculatum. The Structures Of The New Compounds (1-4) Were Elucidated By A Combination Of Spectroscopic Analysis (1-5),Chemical Modifications,And Single-Crystal X-Ray Analysis (1).
Doi:10.1021/np200789S

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专利信息


专利号:US-7589170-B1
优先权日:1998-09-25
标题 :Synthesis of cyclic peptides
发明人:SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER
权利人:UNIV QUEENSLAND
摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.

专利号:WO-9201667-A1
优先权日:1990-07-25
标题 :Renal-selective prodrugs for control of renal sympathetic nerve activity in the treatment of hypertension
发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
权利人:SEARLE & CO
摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kydney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase-inhibitors, of which N-acetyl-η-glutamyl fusaric acid hydrazide [represented in formula (a)] is preferred.

专利号:US-2024026314-A1
优先权日:2020-11-25
标题 :Polypeptides for use in the synthesis of bioactive phenolic compounds
发明人:ROTHSTEIN STEVEN; AKHTAR TARIQ; CASARETTO JOSE; PERRIN COLBY; VAN GELDER KRISTEN
权利人:ROTHSTEIN STEVEN; AKHTAR TARIQ; CASARETTO JOSE; PERRIN COLBY; VAN GELDER KRISTEN
摘要:Described herein is a polypeptide encoding a prenyltransferase for prenylating a polyphenol and a polypeptide encoding an O-methyltransferase for methylating a polyphenol. For example, the polypeptide comprises or consists of the sequence of SEQ ID NO: 1, 2, 3, 4, 5, and/or 6, and/or a polypeptide listed in Table 1, and/or SEQ ID NO: 7-30, or a variant thereof having at least 80% sequence identity to SEQ ID NO: 1, 2, 3, 4, 5, and/or 6, and/or the polypeptide listed in Table 1, and/or SEQ ID NO: 7-30, or a fragment of the polypeptide or the variant thereof.

专利号:US-11746364-B2
优先权日:2018-01-17
标题 :Enzymatic synthesis of kavalactones and flavokavains
发明人:PLUSKAL TOMÃ?S; Weng jing-ke
权利人:WHITEHEAD INST BIOMEDICAL RES
摘要:Disclosed are methods, compositions, proteins, nucleic acids, cells, vectors, compounds, reagents, and systems for the preparation of kavalactones, flavokavains, and kavalactone and flavokavain biosynthetic intermediates using enzymes expressed in heterologous host cells, such as microorganisms or plants, or using in vitro enzymatic reactions. This invention also provides for the expression of the enzymes by recombinant cell lines and vectors. Furthermore, the enzymes can be components of constructs such as fusion proteins. The kavalactones produced can be utilized to treat anxiety disorder, insomnia, and other psychological and neurological disorders. The flavokavains produced can be utilized to treat various cancers including colon, bladder, and breast cancers.

专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人:MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

专利号:US-9453037-B2
优先权日:2011-07-28
标 题 :Methylphenidate-prodrugs, processes of making and using the same
发明人:GUENTHER SVEN; CHI GUOCHEN; BERA BINDU; MICKLE TRAVIS; BERA SANJIB
权利人:KEMPHARM INC; KEMPHARM INC
摘要:The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
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合成参考文献


参考文献:10.1007/s00394-011-0227-y
摘要:Duchnowicz P, Broncel M, Podsędek A, Koter-Michalak M. Hypolipidemic and antioxidant effects of hydroxycinnamic acids, quercetin, and cyanidin 3-glucoside in hypercholesterolemic erythrocytes (in vitro study). European Journal of Nutrition. 2011 Jul 14;51(4):435–43. doi: 10.1007/s00394-011-0227-y.
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