- 15-ketone preparation method
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The present invention relates to a drug intermediate 15-ketone preparation method in chemical field. The preparation method comprises the following steps: (1) (-)-Corey lactone benzoate, an oxidizing agent and a catalyst are added into a first organic solvent for oxidation to obtain a reaction solution A; (2) after a dilute acid is dropwise added into the reaction solution A obtained in the step (1), the solution is stirred and filtered, the filtrate is extracted directly with the first organic solvent, an organic phase is washed with water, dehydrated with a desiccant and filtered to obtain a (-)-Corey lactone benzoate aldehyde solution; (3) Wittig reagent is added into the (-)-Corey lactone benzoate aldehyde solution obtained in the step (2) for Wittig reaction to obtain a reaction solution B, the reaction solution B is concentrated, a second organic solvent is added, and after cooling and crystallization, a crystallization liquid is obtained; and (4) the crystallization liquid obtained in the step (3) is filtered, the filter cake is washed with a third organic solvent, the filter cake is dissolved by the first organic solvent for impurity removal, and after filteration and concentration, an oil matter is obtained. The drug intermediate 15-ketone preparation method has the advantages of good product quality and the like.
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Paragraph 0014
(2016/10/10)
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- PROSTAGLANDIN E1 AND E2 ANALOGS FOR THE TREATMENT OF VARIOUS MEDICAL CONDITIONS
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A prostaglandin analog with selectivity to EP receptors and demonstrating EP agonist activity that may be used to expand hematopoietic stem cell populations or to treat or prevent influenza, bone fracture, bone disease, glaucoma, ocular hypertension, dysm
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Page/Page column 7
(2009/05/28)
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- Enantio- and stereospecific syntheses of 15(R)-Me-PGD2, a potent and selective DP2-receptor agonist
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(Chemical Equation Presented) The first total synthesis of 15(R)-Me-PGD2 3 is reported. The synthesis is based on the enantioselective and stereospecific syntheses of synthon 17 and its attachment to the five-membered ring by a olefin cross metathesis reaction. This approach permits the introduction of a side chain with a predetermined stereogenic center into the prostanoid ring, resulting in the synthesis of 15R-methyl prostaglandin D2 and allows rapid access to other prostanoids.
- Patel, Pranav,Lee, Gue-Jae,Kim, Seongjin,Grant, Gail E.,Powell, William S.,Rokach, Joshua
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supporting information; scheme or table
p. 7213 - 7218
(2009/05/26)
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- Method for preparing prostaglandin derivative
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Disclosed is a method for preparing a prostaglandin derivative of formula (A): which comprises reacting an aldehyde represented by formula (1): with a 2-oxoalkyl phosphonate in a reaction solvent under the presence of alkali hydroxide as sole base. By carrying out the reaction using an alkali hydroxide as sole base in the reaction system, the desired prostaglandin derivative can be obtained by simple procedures and with high yield.
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Page/Page column 14-15
(2010/11/28)
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- Synthesis of 15R-PGD2: A potential DP2 receptor agonist
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The first total synthesis of 15R-PGD2 3 was accomplished. The approach used in this report is also an efficient method to produce 15R-PGE 2. 15R-PGD2, a potential DP2 receptor agonist, could be an important novel tool for defining the role of this receptor in inflammatory diseases.
- Kim, Seongjin,Bellone, Sophie,Maxey, Kirk M.,Powell, William S.,Lee, Gue-Jae,Rokach, Joshua
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p. 1873 - 1876
(2007/10/03)
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- First enantioselective total synthesis of (8S,12R,15S)-prostaglandin J2
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Enantioselective synthesis of natural PGJ2 has been accomplished for the first time starting from the commercially available enantiopure aldehyde 7 in 10% overall yield. The key reaction was a novel prostaglandin class interconversion, i.e., an
- Zanoni, Giuseppe,Porta, Alessio,de Toma, Quintino,Castronovo, Francesca,Vidari, Giovanni
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p. 6437 - 6439
(2007/10/03)
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