- Preparation method of beta-carboxyl phosphate
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The invention provides a preparation method of beta-carboxyl phosphate. The preparation method comprises the following steps: carrying out regional selective ring-opening reaction on an epoxy compound and trialkyl phosphite to generate beta-carboxyl phosphate intermediate; and then oxidizing the beta-carboxyl phosphate intermediate to obtain the beta-carboxyl phosphate. The method is gentle in reaction condition and simple and convenient to operate without protection of an anhydrous solvent and oxygen, and is suitable for large-scale production. The beta-carboxyl phosphate synthesized by the preparation method can be used as an important intermediate synthesized by various misoprostols, such as travoprost, bimatoprost and tafluprost.
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Paragraph 0075; 0082; 0083; 0104; 0105; 0106; 0107
(2017/09/01)
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- Novel method for preparing Prostaglandin derivatives
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Provided is a novel method for preparing prostaglandin derivatives. The method is suitable for mass production by effectively manufacturing prostaglandin derivatives with high yield. The method comprises the following steps: (S-1) adding a first reducing agent to a prostaglandin intermediate compound represented by chemical formula II and manufacturing a compound represented by chemical formula III; (S-2) manufacturing a compound represented by chemical formula IV from the compound represented by chemical formula III in the presence of a base; (S-3) adding a second reducing agent to the compound represented by chemical formula IV and manufacturing a compound represented by chemical formula V; and (S-4) performing Wittig reaction of the compound represented by chemical formula V and a compound represented by chemical formula VI, and manufacturing a compound represented by chemical formula I.COPYRIGHT KIPO 2017
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Paragraph 0136; 0137; 0142-0144
(2017/10/31)
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- Synthesis of (±) travoprost and its analogs
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A new synthetic approach for the antiglaucoma agent, travoprost (1) has been developed in four steps from key intermediate (2). Key transformations include Horner-Wadsworth-Emmons reaction and separation of diastereomers to obtain (±) travoprost (1) and its analogs.
- Mudduluru, Harikrishna,Hindupur, Rama M.,Dubey, Pramod K.,Madhavaram, Shankar,Tatini, Lakshmikumar,Subbaraju, Gottumukkala V.
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experimental part
p. 234 - 241
(2012/04/18)
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- PROCESS FOR THE PREPARATION OF F-SERIES PROSTAGLANDINS
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A process for the synthesis and purification of F-series prostaglandin compounds and synthetic intermediates used to prepare them. The synthetic intermediates are solid and may be purified by precipitation and therefore may form the representative F-series prostaglandin compounds such as latanoprost, bimatoprost, fluprostenol, cloprostenol, and substituted analogs therefrom in highly pure forms.
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Page/Page column 59-60
(2011/05/05)
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- Process for the preparation of prostaglandin derivatives
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The invention provides a novel process for the preparation of prostaglandins and analogues thereof, and new crystalline intermediates in the process.
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- 16-Phenoxy and phenylthio prostaglandin derivatives
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The present invention relates to compounds of the formula: STR1 wherein A represents a grouping of the formula: STR2 B represents an oxygen or sulphur atom, R1 and R2, which may be the same or different, each represent a hydrogen or halogen atom, a trifluoromethyl group, or a straight- or branched-chain alkyl or alkoxy group containing from 1 to 4 carbon atoms, R represents a group of the formula --COOR3, in which R3 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, or a group of the formula --CH2 OR4, in which R4 represents a hydrogen atom or an alkylcarbonyl group containing from 2 to 5 carbon atoms and the double bonds depicted in positions C2 -C3, C5 -C6 and C13 -C14 are trans, cis and trans respectively, the cyclodextrin clathrates thereof and, when R3 in the group --COOR3 represents a hydrogen atom, non-toxic salts thereof. These compounds exhibit characteristics of prostaglandin-like activity.
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- Aldehyde derivatives of prostaglandins
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Prostaglandin analogues of the formula:- SPC1 Wherein A represents a PGF or PGE grouping, X represents ethylene or cis-vinylene, Y represents ethylene or transvinylene, R1 represents hydrogen or alkyl of 1 to 4 carbon atoms, R2 represents alkyl of 1 to 10 carbon atoms, or alkyl of 1 to 4 carbon atoms substituted by phenyl or cycloalkyl containing from 5 to 7 carbon atoms, or R2 represents a grouping of the formula:- SPC2 Wherein R3 represents alkylene of 1 to 4 carbon atoms, R4 represents oxygen or sulphur or sulphinyl, and R5 and R6 represent hydrogen, halogen, trifluoromethyl, alkyl of 1 to 3 carbon atoms are new compounds possessing pharmacological properties.
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- 16-Phenoxy and 16-substituted phenoxy-prostatrienoic acid derivatives
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Novel racemic and 8R-antimeric 16-phenoxy- and 16-(o, m or p)-substituted phenoxy derivatives of 9α, 11α,15-trihydroxy-17,18,19,20-tetranorprosta-4,5,13-trans-trienoic acids, which may be further substituted at C-15 by a methyl or ethyl group, the pharmaceutically acceptable, non-toxic lower alkyl esters and salts thereof and processes for the production of such compounds. dl 9α,11α,15α-trihydroxy-16-m-trifluoromethylphenoxy-17,18,19,20-tetranorprosta-4,5,13-trans-trienoic acid and dl 9α,11α,15 -trihydroxy-15 -methyl-16-m-trifluoromethylphenoxy-17,18,19,20-tetranorprosta-4,5,13-trans-trienoic acid are representative compounds of the class. These compounds possess prostaglandin-like activities and thus are useful in the treatment of mammals where prostaglandins are indicated. They are particularly useful as luteolytic agents in female mammals.
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