CAS: 28416-82-2; (6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-Difluoro-11,17-Dihydroxy-10,13,16-Trimethyl-3-Oxo-6,7,8,9,10,11,12,13,14,15,16,17-Dodecahydro-3H-Cyclopenta[a]Phenanthrene-17-Carboxylic Acid (Fluticasone Impurity)

上下游产品

CAS号2135-17-3 氟米松 | CAS号80474-45-9 氟替卡松丙酸酯中间体 E | CAS号80474-14-2 氟替卡松丙酸酯 | CAS号80473-92-3 (6A,11B,16A,17A... | CAS号65429-42-7 6Α,9Α-二氟-11Β-羟基... | CAS号73205-13-7 氟替卡松丙酸酯USP杂质D

氟米松置于高碘酸体系中,用 1,4-二氧六环,水 用作溶剂,化学反应 2.0H,反应生成6,9-二氟-11,17-二羟基-16-甲基-3-氧代雄甾-1,4-二烯-17-羧酸
参考文献:大环内酯类:一类新型的抗炎化合物
标题:大环内酯类:一类新型的抗炎化合物
摘要:通过将有效的糖皮质激素类固醇与大环内酯类化合物结合在一起,引入了安全糖皮质激素治疗设计的新概念.这些化合物是由9-Deokso-9A-Aza-9A-同反霉素a和3-Descladinosyl-9-Deokso-9A-Aza-9A-的各种类固醇17β-羧酸和9A-N-(3-氨基烷基)衍生物合成的使用稳定的烷基链的同型阿霉素.结合大环内酯类化合物优先在免疫细胞(特别是吞噬细胞)中积累的特性与经典类固醇的抗炎活性,我们设计了在卵白蛋白(ova)诱导的哮喘大鼠中表现出非常好抗炎活性的分子.描述了这种新型化合物的合成,体外和体内抗炎活性.
Doi:10.1016/j.Bmc.2012.10.036

专利信息

专利号:US-7208613-B2
优先权日:2002-06-20
标 题:Synthesis of s-fluoromethyl 6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-propionyloxy-3-oxoandrosta-1,4-diene-17β-carbothioate
发明人：JADAV KANAKSINH JESINGBHAI; KAMBHAMPATI SUDHAKAR; CHITTURI TRINADHA RAO; THENNATI RAJAMANNAR
权利人:SUN PHARMACEUTICAL IND LTD
摘要:The present invention provides a convenient process for the preparation of S-fluoromethyl 6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-propionyloxy-3-oxoandrosta-1,4-diene-17β-carbothioate, a compound of formula 1, comprisingn (a) treating 17β-[(N,N-dimethylcarbamoyl)thio]carbonyl-6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-propionyloxy-3-oxoandrosta-1,4-diene, a compound of formula 3 with alkali metal carbonate-alcohol system to obtain 6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-propionyloxy-3-oxoandrosta-1,4-diene-17β-carbothioic acid, a compound of formula 4; (b) reacting the compound of formula 4 with bromofluoromethane to yield the compound of formula 1.

专利号:US-8344168-B2
优先权日:2006-06-14
标题 :Process for the preparation of fluticasone propionate
发明人：GORE VINAYAK G; GADAKAR MAHESH; POKHARKAR K; WAKCHURE V
权利人:GENERICS UK LTD; GORE VINAYAK G; GADAKAR MAHESH; POKHARKAR K; WAKCHURE V
摘要:The present invention relates to a process for the preparation of steroidal 17β-carboxylic thioates. More particularly the present invention relates to a convenient and efficient synthesis of steroidal 17β-carboxylic thioates, such as fluticasone propionate I, using soluble mixed fluorides to introduce fluorine by displacing an appropriate leaving group X in compounds II resulting in selective and controlled fluorination. The present invention also relates to intermediates II and their preparation.

专利号:US-7214807-B2
优先权日:2000-02-25
标 题 :Method for the preparation of fluticasone and related 17β-carbothioic esters using a novel carbothioic acid synthesis and novel purification methods
发明人：BARKALOW JUFANG; CHAMBERLIN STEVEN A; COOPER ARTHUR J; HOSSAIN AZAD; HUFNAGEL JOHN J; LANGRIDGE DENTON
权利人:ABBOTT LAB
摘要:This invention discloses a novel method for the conversion of carboxylic acids to carbothioic acids and application of the method to the preparation of androstane carbothiolates, such as fluticasone propionate, which avoids column chromatography.

专利号:US-2005256325-A1
优先权日:2002-06-20
标题:Convenient synthesis of s-fluoromethyl 6alpha, 9alpha-difluoro-11beta-hydroxy-16alpha-methyl-17alpha-propionyloxy-3-oxoandrosta-1,4-diene-17beta-carbothioate

专利号:JP-2003529564-A
优先权日:2000-02-25
标 题 :Process for the preparation of fluticasone and related 17.beta.-carbothioates using a novel method of synthesis and a novel purification method of carbothioic acid

专利号:US-2004209854-A1
优先权日:2000-02-25
标 题:Method for the preparation of fluticasone and related 17beta-carbothioic esters using a novel carbothioic acid synthesis and novel purification methods