- Preparation method of tafluprost
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The invention provides a preparation method of tafluprost. According to the method, a fluorinated raw material is obtained at first, and then, HWE reaction is carried out to form double bonds; and therefore, the double bond addition side reaction during fluorination can be avoided. Therefore, the method disclosed by the invention can be used for obtaining the fluorinated product with high yield and high purity, so that the preparation cost of the tafluprost can be reduced, and the economic benefit of the tafluprost can be improved.
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- METHOD OF PURIFICATION OF PROSTAGLANDINS INCLUDING FLUORINE ATOMS BY PREPARATIVE HPLC
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The present invention discloses a method of purification of prostaglandins including fluorine atoms by using preparative HPLC. Tafluprost and Travoprost are prostaglandins including fluorine. The chemical structure of the impurities in crude Tafluprost an
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Paragraph 0016
(2014/03/24)
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- AMINE SALTS OF PROSTAGLANDIN ANALOGS
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The present application relates to amine salts of prostaglandin analogs and their uses for the preparation of substantially pure prostaglandin analogs. Specific embodiments relate to amine salts of tafluprost and their uses for the preparation of substant
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Page/Page column 8
(2013/08/28)
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- Synthesis and biological properties of novel fluoroprostaglandin derivatives: Highly selective and potent agonists for prostaglandin receptors
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Synthesis of novel 7,7-difluoroprostacyclin and 15-deoxy-15,15-difluoro- PGF2α derivatives will be presented. These compounds show high affinity to prostaglandin receptors and potent biological activities.
- Matsumura, Yasushi,Nakano, Takashi,Mori, Nobuaki,Morizawa, Yoshitomi
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p. 148 - 152
(2007/10/03)
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- Synthesis of the highly potent prostanoid FP receptor agonist, AFP-168: A novel 15-deoxy-15,15-difluoroprostaglandin F2α derivative
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A novel 15-deoxy-15,15-difluoro-prostaglandin(PG)F2α derivative 6 (AFP-168) has been synthesized from the Corey aldehyde in six steps. A key aspect of this route is difluorination of an enone and a stereoselective Wittig reaction. The compound shows high affinity to the FP receptor and potent activities for an anti-glaucoma agent.
- Matsumura, Yasushi,Mori, Nobuaki,Nakano, Takashi,Sasakura, Hideshi,Matsugi, Takeshi,Hara, Hideaki,Morizawa, Yoshitomi
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p. 1527 - 1529
(2007/10/03)
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- Difluoroprostaglandin derivatives and their use
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A fluorine-containing prostaglandin derivative of the formula (1) (or a salt thereof) and a medicine containing it, particularly, a preventive or therapeutic medicine for an eye disease: STR1 wherein A is a vinylene group or the like, R1 is an
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