CAS: 496-63-9; 3-Hydroxy-4H-Pyran-4-One

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644-46-2 118-71-8 7559-81-1

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CAS号61049-67-0 维达列汀 | CAS号1219-33-6 5-苄氧基-4-氧代-4H-吡... | CAS号98-00-0 糠醇 | CAS号73322-54-0 O-Acetylpyromec... | CAS号19969-71-2 2,5-二氢-2,5-二甲氧基糠基醇 | CAS号60249-17-4 6-甲氧基-2,6-二氢-3H... | CAS号74425-84-6 4-Bromo-6-metho... | CAS号501-30-4 曲酸 | CAS号15771-06-9 5-(苄氧基-2-(羟甲基)-... | CAS号135593-77-0 1,3,4-tri-O-ace... | CAS号1064077-34-4 1-甲基-3-(苯甲氧基)-4... | CAS号857054-02-5 Karrikinolide | CAS号89282-30-4 3-hydroxypyran-... | CAS号61049-67-0 维达列汀

📜糠醇置于sodium Acetate,氯体系中,用 乙醇,水 作为反应溶剂,以62%的收率获得产物3-羟基-4H-吡喃-4-酮
参考文献:一种3-(苄氧基)-4-氧代-4H-吡喃-2-羧酸的合成方法
标题:一种3-(苄氧基)-4-氧代-4H-吡喃-2-羧酸的合成方法
摘要:本发明公开了一种3‑(苄氧基)‑4‑氧代‑4H‑吡喃‑2‑羧酸的合成方法,以糠醇为起始原料,经过重排,加成,羟基保护,氧化四步反应,本发明的合成路线总摩尔收率大于32%,具有反应条件相对温和等特点,显著提高了3‑(苄氧基)‑4‑氧代‑4H‑吡喃‑2‑羧酸的收率和纯度,同时本发明工艺操作步骤详细,参数具体,条件可控,工艺稳定,可工业化大批量生产.

专利信息

专利号:US-7816544-B2
优先权日:2004-03-23
标 题:Synthesis of rocaglamide natural products via photochemical generation of oxidopyrylium species
发明人：JONES II GUILFORD; GERARD BAUDOUIN; PORCO JR JOHN A
权利人:UNIV BOSTON
摘要:The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.

专利号:US-8404088-B2
优先权日:2006-05-22
标 题:Asymmetric synthesis of rocaglamides via enantioselective photocycloaddition mediated by chiral bronsted acids
发明人：PORCO JR JOHN A; GERARD BAUDOUIN
权利人:PORCO JR JOHN A; GERARD BAUDOUIN; UNIV BOSTON
摘要:The present invention provides a new strategies for the synthesis of compounds of the rocaglamide family and related natural products. The synthetic approach generally involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by an enantioselective 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile in the presence of a TADDOL derivative. This approach can be used for the formation of adducts containing an aglain core structure. Methods of the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.

专利号:US-2004101523-A1
优先权日:1989-07-27
标题:Renal-selective prodrugs for control of renal smpathetic 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 kidney. 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-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.

专利号:WO-9101724-A1
优先权日:1989-07-27
标题 :Renal-selective prodrugs for 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 depa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitors 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 kidney. 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-Y-glutamyl fusaric acid is preferred.

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-6177409-B1
优先权日:1996-07-05
标 题 :Method for the site specific synthesis of novel 3-hydroxypyridin-4(1H)ons derivatives from aminomonosaccharides or aminoitols, products obtained by this method and their applications
发明人：VANLEMMENS PIERRE PAUL; POSTEL DENIS GHISLAIN; GERMAIN PIERIG EMMANUEL; JULIEN RENE JEAN-MARIE; PETIT JEAN-PIERRE CONSTANT; RONCO GINO LINO; VILLA PIERRE JOSEPH
权利人:INST BIOCHIMICO PAVESE PHARMA
摘要:Process for regiospecific preparation of new 3-hydroxypyridine-4(1H)-one derivatives starting from monosaccharides or itols of general formula:in which R represents a radical, either saturated or not, branched or not, having carbon-atom groups, and having hetero-atoms or not, and Sub represents a saccharide derivative or an itol, either cyclic not, protected or not, the hydrocarbon skeleton of which is bound to the nitrogen atom of the pyridinone either directly or by the intermediary of a spacing group. The present invention is characterized in that the process comprises a first step of protection of the 3-hydroxy group of the pyranone derivative, a second basocatalyzed step of substitution of the intracyclic oxygen atom of the pyranone by the nitrogen atom of the amine function of the amino monosaccharide or amino itol, and a third step of de-protection of the 3-OH group of the pyridinone cycle and possibly of the OH groups of the glucide or itol residue. It also regards the products obtained by this process, as well as their applications, namely as medicaments for the treatment of toxic overloads of FeIII.