- He fluorine front row element intermediate preparation method (by machine translation)
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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)
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Paragraph 0034; 0035; 0036
(2018/05/16)
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- 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 0086; 0089; 0090
(2017/09/01)
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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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p. 234 - 241
(2012/04/18)
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- PROSTANOIDS. XXX. SYNTHESIS OF THE ANALOGS OF 11-DEOXYPROSTA-GLANDINS E AND F
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A practical approach to 11-deoxyprostaglandins is developed on the basis of the chemo- and stereoselective reduction of the readily obtainable methyl 9,15-diketo-16-aryloxyprostenoates.
- Tolstikov, G. A.,Miftakhov, M. S.,Adler, M. E.,Platonov, V. E.,Sagitdinova, Kh. F.,Khalilov, L. M.
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p. 100 - 107
(2007/10/02)
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- 2,5,6,7-tetranor-4,8-inter-m-phenylene PGI2 derivatives
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Disclosed herein are novel prostaglandin I2 (PGI2) derivatives exhibiting excellent in vivo duration and activities, said derivatives being represented by the general formula: STR1 wherein R1, X, R2 and R3 are as defined herein.
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- 9-Substituted carbacyclin analogs
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Novel compounds of the following formula: STR1
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- 9-Substituted carbacyclin analogs
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Novel compounds of the following general formula: STR1
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- 9-Substituted carbacyclin analogs
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Novel compounds of the following general formula: STR1
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- Method of inducing luteolysis using 16-aryloxy-17,18,19,20-tetranor-prostanoic acid derivatives
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The disclosure relates to novel 17,18,19,20-tetranor-prostanoic acid derivatives having prostaglandin-type properties, to a method for their manufacture, and also to pharmaceutical or veterinary compositions containing said novel derivatives and a method of inducing luteolysis in an animal host by use of said novel derivatives.
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- N-(Methanesulfonyl)-16-phenoxyprostaglandincarboxamides: Tissue-Selective, Uterine Stimulants
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In an effort to develop tissue-selective prostaglandin analogues resistant to the metabolic inactivating pathways of the natural materials, hybrid compounds modified both at C-1 with a sulfonimide moiety and in the n-amylcarbinol side chain with substituted phenoxy groups were synthesized and evaluated in a variety of in vitro and in vivo models.Several of these analogues exhibited potent, tissue-selective, uterine stimulant activity, a finding subsequently confirmed in clinical studies with one member of this series, N-(methanesulfonyl)-16-phenoxy-ω-tetranor-PGE2-carboxamide (CP-34089/ZK-57671, sulprostone).
- Schaaf, Thomas K.,Bindra, Jasjit S.,Eggler, James F.,Plattner, Jacob J.,Nelson, A. James,et al.
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p. 1353 - 1359
(2007/10/02)
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- 16-Phenoxy prostaglandin A2 analogs
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Prostaglandin-type compounds with a phenoxy or substituted-phenoxy substituent at the C-16 position are disclosed, with processes for making them. These compounds are useful for a variety of pharmacological purposes, including anti-ulcer, inhibition of platelet aggregation, increase of nasal patency, labor inducement at term, and wound healing.
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- 11-Deoxy-cis-4,5-didehydro-ω-aryl-PGE compounds
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11-Deoxy prostaglandin type compounds, i.e. prostaglandin type compounds in which the 11-hydroxy group is replaced by hydrogen, are disclosed, with processes for making them. These compounds are useful for a variety of pharmacological purposes, including anti-ulcer, inhibition of platelet aggregation, increase of nasal patency, and labor induction at term. This is a division of application Ser. No. 609,410, filed Sept. 2, 1975.
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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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- 5-(2-Carboxythiophen-5-yl)-16-aryloxy-α-tetranor-ω-tetranorprostaglandins
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5-(2-Carboxythiophen-5-yl)-16-aryloxy-α-tetranor-ω-tetranorprostaglandins and intermediates useful in their preparation are disclosed. The novel prostaglandins of this invention have been found to have activity profiles comparable to the parent prostaglandins but they exhibit a greater tissue specificity of action.
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- Substituted ω-pentanorprostaglandins
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Substituted novel ω-pentanorprostaglandins and various novel intermediates and reagents used in their preparation.
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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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- Synergistic composition comprising PGF2α and PGE2
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A synergistic composition comprising as active ingredients a PGF2α compound or its cyclodextrin clathrate thereof and a PGE2 compound or its cyclodextrin clathrate thereof, at a weight ratio of from about 1:0.33 to about 1:1.
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