CAS: 536-69-6; 5-Butylpicolinic Acid

上下游产品

Methyl 5-Butylpicolinate 17072-92-3
Ethyl 5-Butylpicolinate 17072-93-4
Tert-Butyl 5-Butyrylpyridine-2-Carboxylate 165275-94-5
Benzyl 5-N-Butylpyridine-2-Carboxylate 130412-69-0
1-(5-Butyl-Pyridin-2-yl)-Ethanone 68520-81-0
Tert-Butyl 5-Butyrylpyridine-2-Carboxylate 165275-93-4
5-丁基-2-甲基吡啶 5-Butyl-2-Methylpyridine 702-16-9
5-N-Butyl-2-Cyanopyridine 39256-40-1
5-丁基-2-丙基-吡啶 5-Butyl-2-Propyl-Pyridine 21192-17-6
2,5-二丁基吡啶 2,5-Dibutyl-Pyridine 112945-05-8

Tert-Butyl 5-Butyrylpyridine-2-Carboxylate置于盐酸体系中,用 四氢呋喃 作为反应溶剂,化学反应 3.0H,以93%的收率获得产物5-丁基吡啶-2-羧酸
参考文献:Carbon Functionalizations On Pyridine Ring Via Trimethylstannyl Derivatives-An Example Of Fusaric Acid Synthesis-
标题:Carbon Functionalizations On Pyridine Ring Via Trimethylstannyl Derivatives-An Example Of Fusaric Acid Synthesis-
摘要:Method For Introduction Of Two Types Of Carbon Functional Groups,Acyl And Tert-Butoxycarbonyl Groups,In Pyridine Ring Via Bis(Trimethylstannyl) Pyridine (1) Is Explored. Application Of This Method To The Synthesis Of Fusaric Add (11) Is Also Described.
DOI:10.3987/com-94-7012

专利信息

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-2004053355-A1
优先权日:2000-05-26
标题:Modular approach to on-line synthesis, drug discovery and biochemical transformations using immobilized enzyme reactors
发明人：WAINER IRVING; MARKOGLOU NEKTARIA
摘要:A coupled system using extremely different enzymes with incompatible cofactors and reaction conditions has been constructed using standard liquid chromatographic formats and open tubular formats. One of the significant aspects of the present invention lies in the development of the liquid chromatographic on-line enzyme cascade. This has been illustrated by the biosynthetic pathway involving dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase which encompass the synthesis of the key neurotransmitters, norepinephrine and epinephrine. The results demonstrate for the first time the immobilization of dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase. The IMERs are active and can be used in a liquid chromatographic format for qualitative and quantitative determinations. The IMER-HPLC system can be used to carry out standard Michaelis-Menten enzyme kinetic studies and to quantitatively determine enzyme kinetic constants, identify specific enzyme inhibitors, provide information regarding the mode of inhibition and the inhibitor constants (K i ). A second significant aspect of the present invention lies in the ability of the immobilized enzyme reactors to be used independently or as a combination, thus providing a unique opportunity to explore the interrelationships between these enzymes, to investigate the source of diseases and to design new drug entities for identified clinical syndromes.

专利号:WO-2024262824-A1
优先权日:2023-06-20
标 题 :Novel process for synthesis of polysubstituted pyridine derivatives
发明人：PARK SEUNG BUM; YI SIHYEONG
权利人:SEOUL NAT UNIV R&DB FOUNDATION
摘要:The present invention relates to a novel method for synthesizing a polysubstituted pyridine derivative and, more specifically, to a method for synthesizing a 2,3,5-substituted pyridine derivative through a specific ring cleavage reaction. In the synthesis method of the present invention, an enamine structure is formed in situ by using beta keto ester/sulfone/phosphonic acid ester and ammonium acetate and subjected to an aldol condensation reaction with 3-formyl (aza) indole/benzofuran, a cyclization reaction, and a ring-cleavage reaction in that order to synthesize a characteristic pyridine structure having an alkyl/aryl substituent attached to the 2-position thereof, an ester/sulfone/phosphonic acid ester attached to the 3-position thereof, and ortho-aminoaryl/phenol including various substituents attached to the 5-position thereof. In particular, (aza)indole/benzofuran and beta keto ester/sulfone/phosphonic acid ester, which are reaction substrates, are substrates having very high accessibility, and enable the introduction of various substituents, thereby constructing a pyridine skeleton having high biocompatibility into which ortho-aminoaryl or phenol substituents having various substituents are introduced.

专利号:US-5200341-A
优先权日:1991-10-07
标 题:Altered gene and E. coli strains and methods useful in enhanced accumulation of proteins
发明人：OBUKOWICZ MARK G
权利人:MONSANTO CO
摘要:An rpoH gene that encodes a sigma 32 protein in which cysteine instead of arginine is at amino acid residue 268 was isolated from a mutant of Escherichia coli strain W3110. The rpoH gene has thymine instead of cytosine at the nucleotide position corresponding to 802 in the wild-type rpoH gene. Purified strains of E. coli W3110 and JM101 having a mutant rpoH gene in which thymine instead of cytosine is at the nucleotide position corresponding to 802 in a wild-type rpoH gene and a method for synthesis of proteins at enhanced levels are also disclosed. The method comprises introducing an expression vehicle into an E. coli strain containing the mutant rpoH gene of this invention.