CAS: 40034-42-2; 1-Ethyl-4-Oxo-7-(Pyridin-4-yl)-1,4-Dihydroquinoline-3-Carboxylic Acid

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CAS号40034-46-6 ethyl 1-ethyl-1... | CAS号40034-44-4 3-吡啶-4-基苯胺 | CAS号40034-45-5 diethyl 2-[(3-p... | CAS号40034-41-1 ethyl 1,4-dihyd...

📜3-Acetyl-1-Ethyl-1,4-Dihydro-4-Oxo-7-(Pyridin-4-yl)Quinoline 反应生成 罗索沙星
参考文献:Alkyl .Alpha.-[3-(Pyridyl)-Anilinomethylene]Acetoacetates
标题:Alkyl .Alpha.-[3-(Pyridyl)-Anilinomethylene]Acetoacetates
摘要:将3-Py-苯胺(i)与低烷基乙酰乙酸酯(II)和三-(低烷基)正甲酸酯(iii)反应,反应生成低烷基 .Alpha.-(3-Py-苯胺亚甲基)乙酰乙酸酯(iv),加热低烷基 .Alpha.-(3-Py-苯胺亚甲基)乙酰乙酸酯(iv),反应生成3-乙酰基-1,4-二氢-4-氧基-7-Py-喹啉(v),它与3-乙酰基-4-羟基-7-Py-喹啉(va)互变异构,将v(或va)与一种低烷基化试剂反应,反应生成3-乙酰基-1-(低烷基)-1,4-二氢-4-氧基-7-Py-喹啉(vi),并将vi转化为1-(低烷基)-1,4-二氢-4-氧基-7-Py-3-喹啉羧酸(vii),其中py是4(或3)-吡啶基或带有一个或两个低烷基取代基的4(或3)-吡啶基.公式vii的化合物是已知的抗菌剂.

专利信息

专利号:US-4699984-A
优先权日:1984-09-17
标 题 :Preparation of intermediates to 6-fluoro-7-(2,6-dimethylpyridyl)quinoline carboxylic acids and compounds
发明人：SINGH BALDEV
权利人:STERLING DRUG INC
摘要:Shown is the process which comprises heating 4-(2-fluorophenyl)-2,6-dimethyl-3,5-pyridinedicarboxylic acid to produce a mixture of 4-(2-fluorophenyl)-2,6-dimethylpyridine and 2,4-dimethyl-5H-[1]benzopyrano[3,4-c]pyridin-5-one, separating the components of said mixture and nitrating 4-(2-fluorophenyl)-2,6-dimethylpyridine to produce 4-(2-fluoro-5-nitrophenyl)-2,6-dimethylpyridine. Also shown are the 3-step synthesis of 4-(2-fluorophenyl)-2,6-dimethyl-3,5-pyridinedicarboxylic acid from 2-fluorobenzaldehyde and the five step synthesis of 1-ethyl-6-fluoro-1,4-dihydro-7-(2,6-dimethyl-4-pyridinyl)-4-oxo-3-quinolinecarboxylic acid, a highly potent antibacterial agent, starting with 4-(2-fluoro-5-nitrophenyl)-2,6-dimethylpyridine. Other intermediates shown in said five step synthesis include 3-(2,6-dimethyl-4-pyridinyl)-4-fluorobenzeneamine and diethyl 4-fluoro-3-(2,6-dimethyl-4-pyridinyl)anilinomethylenemalonate.

专利号:US-8017776-B2
优先权日:2003-07-15
标题 :Methods for synthesis of acyloxyalkyl compounds
发明人：BHAT LAXMINARAYAN; GALLOP MARK A
权利人:XENOPORT INC
摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

专利号:US-9693999-B2
优先权日:2011-01-26
标题:Small molecule RNase inhibitors and methods of use
发明人：DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE
权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education
摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.

专利号:US-8143437-B2
优先权日:2002-02-19
标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
发明人：GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X
权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC
摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

专利号:US-2010203587-A1
优先权日:2009-01-13
标 题:Use of dna gyrase inhibitors for in vitro polypeptide synthesis reactions
发明人：VOLOSHIN ALEXEI M; ZAWADA JAMES F; GOLD DANIEL
权利人:SUTRO BIOPHARMA INC
摘要:The present invention provides methods and compositions useful for in vitro polypeptide synthesis reactions. The methods involve the use of DNA gyrase inhibitors to prevent bacterial contamination in lysates used for in vitro production of polypeptides. The compositions include contamination-free cell lysates for in vitro protein synthesis reactions.

专利号:WO-2009056955-A1
优先权日:2007-10-30
标题 :Amine-bearing phospholipids (abps), their synthesis and use
发明人：ZUMBUEHL ANDREAS
权利人:UNIV BASEL; ZUMBUEHL ANDREAS
摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.