CAS: 6246-46-4; Ursonic Acid

上下游产品

熊果酸 Ursolic Acid 77-52-1
熊果酸乙酸酯 (3β)-3-Acetoxy-Urs-12-En-28-Carboxylic Acid 7372-30-7
Urs-12-En-3,28-Diol 987-94-0

📜熊果酸置于pyridinium Chlorochromate体系中,用 二氯甲烷,丙酮 作为反应溶剂,化学反应生成 3-氧代-12-烯-28-乌苏酸
参考文献:作为抗锥虫新药的 C3 半合成三萜酯的设计,合成和生物活性
标题:作为抗锥虫新药的 C3 半合成三萜酯的设计,合成和生物活性
摘要:创新药物的研究对于控制和根除寄生虫感染至关重要.受天然抗原虫三萜的启发,通过一步合成从熊果酸和齐墩果酸中衍生出12 种半合成 3-O-芳基烷基酯库.这些化合物与一组三萜酸一起在锥虫,利什曼原虫和 Wi38 细胞系上进行了测试.结果表明,与母体酸相比,三萜c3酯化保留了抗锥虫活性(ic 50 ~1.6-5.5 μm),同时降低了细胞毒性.当空间位阻基团取代双键或屏蔽酯基团时,酯烷基链的不饱和度会导致有趣的活性损失.乌苏烷/齐墩果烷 C3 羟基化是抗莱什曼尼活性的唯一重要特征.在非洲锥虫病急性小鼠模型上测试了两种候选物:二氢肉桂酰熊果酸和 2-氟苯基丙酰熊果酸,二氢肉桂酰衍生物感染后第 5 天寄生虫血症显着减少.应在体外和体内研究对其他烷基/保护基团的进一步评估.
DOI:10.1002/open.202100159

专利信息

专利号:US-7348436-B2
优先权日:2004-03-02
标题 :Compounds useful for the synthesis of (+)-discodermolide and methods thereof
发明人：MYLES DAVID C; SHAW SIMON JAMES; SUNDERMANN KURT F
权利人:KOSAN BIOSCIENCES INC
摘要:Compounds and methods useful for the synthesis of (+)-discodermolide, a naturally occurring microtubule stabilizing agent useful as an anti-cancer agent.

专利号:US-9556140-B2
优先权日:2013-01-26
标 题 :Approach for synthesis of catechins
发明人：DUGAR SUNDEEP; MAHAJAN DINESH; RAI KUMAR SANTOSH; TRIPATHI VINAYAK; PATIL ISHWAR RAKESH
权利人:SPHAERA PHARMA PRIVATE LTD
摘要:A process for synthesis of enatiomerically pure or enatiomerically enriched or racemic mixture of (+ and/or −) epicatechin and its intermediates, comprising the steps of: (i) obtaining penta-protected quercetin; (ii) reducing the penta-protected quercetin obtained from step (i); (iii) optionally deprotecting the compound of step (ii); (iv) reducing the compound obtained from step (ii) or step (iii) in the presence of a chiral/achiral reducing agent to obtain a chiral intermediate; (v) deprotecting and/or hydrogenation of the chiral intermediate obtained from step (iv) to obtain (−)-epicatechin; (vi) optionally simultaneously deprotecting and by drogenation of the compound obtained from step (ii) to obtain racemic epicatechin.

专利号:US-8691989-B2
优先权日:2008-06-20
标题 :Methods of synthesis of morphinans
发明人：LAWSON JOHN A
权利人:LAWSON JOHN A; PHOENIX PHARMALABS INC
摘要:The disclosure describes morphinan compounds and methods for their synthesis. Preferred methods according to the disclosure allow for large-scale preparation of diastereomerically enriched morphinans. Preferred methods according to the disclosure may also allow for the preparation of diastereomerically enriched morphinans using less time, and/or using fewer reaction steps, and/or providing better yield than previously used methods for preparing morphinans. The methods disclosed herein find utility in synthetic organic chemistry as well as medicinal chemistry.

专利号:US-5612217-A
优先权日:1994-10-25
标 题 :Streptomyces sp. MA 7074 (ATCC 55605) used for microbial synthesis of HIV protease inhibitors
发明人：SHAFIEE ALI; CHEN SHIEH-SHUNG T; ARISON BYRON H; MILLER RANDALL R; GARRITY GEORGE M; HEIMBUCH BRIAN
权利人:MERCK & CO INC
摘要:Biotransformation products of a fermentation with culture MA7074 are potent HIV protease inhibitors. These products are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

专利号:US-6610844-B2
优先权日:1996-12-11
标题:Processes for preparation of 9,11-epoxy steroids and intermediates useful therein
发明人：NG JOHN S; LIU CHIN; ANDERSON DENNIS K; LAWSON JON P; WIECZOREK JOSEPH; KUNDA SASTRY A; LETENDRE LEO J; POZZO MARK J; SING YUEN-LUNG L; WANG PING T; YONAN EDWARD E; WEIER RICHARD M; KOWAR THOMAS R; BAEZ JULIO A; ERB BERNHARD
权利人:SEARLE & CO
摘要:Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula Iwherein-A-A- represents the group -CHR4-CHR5- or -CR4=CR5-;R3, R4 and R5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano and aryloxy;R1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical;-B-B- represents the group -CHR6-CHR7- or an alpha- or beta-oriented group:where R6 and R7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy; andR8 and R9 are independently selected from the group consisting of hydrogen, hydroxy, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy, or R8 and R9 together comprise a carbocyclic or heterocyclic ring structure, or R8 or R9 together with R6 or comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring.

专利号:US-5449795-A
优先权日:1994-02-14
标 题 :Process for synthesis of steroidal allylic tert. alcohols
发明人：HOGENKAMP DERK J
权利人:COCENSYS INC
摘要:A method for the preparation of a steroidal allylic tertiary alcohol is disclosed which involves the deprotonation of a sulfoxide with a strong base which is capable of deprotonating the methine proton which is α to the sulfoxide, in an inert solvent to give the anion; reaction of the anion with a steroidal spiro-2'-oxirane to give a steroidal γ-hydroxysulfoxide; and thermolysis in the presence of a base other than calcium carbonate to give the steroidal allylic tertiary alcohol.