209861-01-8Relevant articles and documents
Method for large-scale preparation of tafluprost
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Paragraph 0019; 0022-0024, (2021/01/24)
The invention discloses a method for industrially preparing tafluprost. The method comprises the following steps: taking Corey lactone as an initial raw material, oxidizing, condensing, fluorinating,deprotecting, reducing, re-condensing, esterifying and r
An Asymmetric Suzuki-Miyaura Approach to Prostaglandins: Synthesis of Tafluprost
Fletcher, Stephen P.,Goetzke, F. Wieland,Ku?era, Roman
, (2020/04/09)
We report the catalytic asymmetric synthesis of Tafluprost (1), a prostaglandin analogue. This synthesis demonstrates a new approach to prostaglandins involving symmetrization and desymmetrization of a racemic precursor to control the absolute and relative stereochemistry of the cyclopentyl core. Key steps include a diastereo- and enantioselective Rh-catalyzed Suzuki-Miyaura reaction of a racemic bicyclic allyl chloride and an alkenyl boronic acid and a regio- and diastereoselective Pd-catalyzed Tsuji-Trost reaction with an enolate surrogate.
He fluorine front row element intermediate preparation method (by machine translation)
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, (2018/05/16)
The invention discloses he fluorine front row element intermediate, i.e. formula 5 compound preparation method, including the use of biphenyl formyl protected Corey lactone as raw materials, through oxidation, HWE connected side chain, fluorinated, hydrolysis of deprotection step. Preparation method of this invention has the operability is strong, stable process, intermediates for the preparation of white powder, good stability. (by machine translation)
METHOD OF PURIFICATION OF PROSTAGLANDINS INCLUDING FLUORINE ATOMS BY PREPARATIVE HPLC
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, (2014/03/24)
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
Synthesis of the highly potent prostanoid FP receptor agonist, AFP-168: A novel 15-deoxy-15,15-difluoroprostaglandin F2α derivative
Matsumura, Yasushi,Mori, Nobuaki,Nakano, Takashi,Sasakura, Hideshi,Matsugi, Takeshi,Hara, Hideaki,Morizawa, Yoshitomi
, p. 1527 - 1529 (2007/10/03)
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.
Synthesis and biological properties of novel fluoroprostaglandin derivatives: Highly selective and potent agonists for prostaglandin receptors
Matsumura, Yasushi,Nakano, Takashi,Mori, Nobuaki,Morizawa, Yoshitomi
, p. 148 - 152 (2007/10/03)
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.
Difluoroprostaglandin derivatives and their use
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, (2008/06/13)
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