CAS: 19562-30-2; 8-Ethyl-5-Oxo-2-(Pyrrolidin-1-yl)-5,8-Dihydropyrido[2,3-D]Pyrimidine-6-Carboxylic Acid

上下游产品

8-乙基-5-氧代-2-吡咯烷-1-基吡啶并[6,5-D]嘧啶-6-羧酸乙酯 6-Ethoxycarbonyl-8-Ethyl-5-Oxo-2-Pyrrolidino-5,8-Dihydro-Pyrido[2,3-D]Pyrimidine 33836-43-0

📜8-乙基-5-氧代-2-吡咯烷-1-基吡啶并[6,5-D]嘧啶-6-羧酸乙酯,Sodium Hydroxide,3-Pyrrolidino-5-Ethyl-5,8-Dihydro-8-Oxopyrido<2.3-B>Pyrazine-7-Carboxylic Acid 以 水 用作溶剂,化学反应生成吡乙酸三氮萘
参考文献:Process For The Preparation Of
标题:Process For The Preparation Of
摘要:制备4-氯-5-烷氧羰基-2-甲氧基嘧啶的过程,其化学式为:##str1## 其中r.Sub.1为1至4个碳原子的低级烷基基团,包括以下步骤:A)在水介质中,与过量的碱金属氢氧化物一起,将o-甲基异脲盐和无机或有机酸的盐与烷基烷氧甲基亚甲基丙二酸酯##str2##缩合,形成相应的5-烷氧羰基-4-羟基-2-甲氧基嘧啶盐,并通过加入无机或有机酸的中和来释放该5-烷氧羰基-4-羟基-2-甲氧基嘧啶,以及##str3## B)将后一化合物悬浮在二甲基甲酰胺中,在室温下与氯化硫酰反应,以形成相应的4-氯-5-烷氧羰基-2-甲氧基嘧啶:##str4##

专利信息

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-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:US-2003180254-A1
优先权日:1995-05-26
标题:Immunologic enhancement with intermittent interleukin-2 therapy
发明人：LANE H CLIFFORD; KOVACS JOSEPH A; FAUCI ANTHONY S
权利人:GOVT OF THE USA AS REPRESENTED
摘要:A method for activating a mammalian immune system entails a series of IL-2 administrations that are effected intermittently over an extended period. Each administration of IL-2 is sufficient to allow spontaneous DNA synthesis in peripheral blood or lymph node cells of the patient to increase and peak, and each subsequent administration follows the preceding administration in the series by a period of time that is sufficient to allow IL-2 receptor expression in peripheral or lymph node blood of the patient to increase, peak and then decrease to 50% of peak value. This intermittent IL-2 therapy can be combined with another therapy which targets a specific disease state, such as an anti-retroviral therapy comprising, for example, the administration of AZT, ddI or interferon alpha. In addition, IL-2 administration can be employed to facilitate in situ transduction of T cells in the context of gene therapy. By this approach the cells are first activated in vivo via the aforementioned IL-2 therapy, and transduction then is effected by delivering a genetically engineered retroviral vector directly to the patient.

专利号:US-7632944-B2
优先权日:2007-01-24
标题 :Quinolone carboxylic acids, derivatives thereof, and methods of making and using same
发明人：HARMS ARTHUR E
权利人:BAUSCH & LOMB
摘要:A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.

专利号:US-8227597-B2
优先权日:2006-10-06
标题 :Quinolone carboxylic acids, derivatives thereof, and methods of making and using same
发明人：HARMS ARTHUR E
权利人:HARMS ARTHUR E; BAUSCH & LOMB
摘要:A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.