- The optically pure sodium alcoholate dextrorotary chlorine forefront of the method for the preparation of
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The invention relates to a preparation method of optically pure dextro cloprostenol sodium. The method comprises the following steps: using the combination of ketonic acid and S-phenylethylamine resolving agent, and carrying out chiral resolution to obtain S-propenylphosphonate with the structural formula of R-ketonic acid; then separating to obtain R-chlorone and preparing to obtain R-cloprostenol sodium. The preparation method has the benefits that the optically pure dextro cloprostenol sodium in the invention is called D-cloprostenol sodium for short, the using amount only needs one third of cloprostenol sodium being a racemic modification in current market, and the pesticide effect is obviously better than cloprostenol sodium with three times of using amount.
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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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- Use of 9-deoxy prostaglandin derivatives to treat glaucoma
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Disclosed are 9-deoxyprostaglandins which are useful in the treatment of glaucoma and ocular hypertension. Some of these 9-deoxyprostaglandins are novel. Also disclosed are ophthalmic, pharmaceutical compositions comprising such prostaglandins.
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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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- PROSTANOIDS. XIX. THE SYNTHESIS OF 14C-LABELED CLOPROSTENOL
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A 1:3400 mixture of 2-14C-labelled methyl bromoacetate with the nonradioactive ester gave labelled dimethoxy-2-oxo-3-(m-chlorophenoxy)phosphonate which was used for the synthesis of 16-14C-labelled cloprostenol by the Corey strategy.
- Miftakhov, M. S.,Vostrikov, N. S.,Kuznetsov, O. M.,Kuvatov, Yu. G.,Murinov, Yu. I.,Tolstikov, G. A.
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p. 1072 - 1075
(2007/10/02)
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- Tertiary alcohols
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Tertiary alcohols of the formula: STR1 wherein Y1 represents a carbonyl or hydroxymethylene group, and either (i) A1 represents a direct bond and R1 represents a phenyl group which may optionally carry one or more substituents selected from halogen atoms, straight- or branched-chain alkyl or alkoxy groups, each containing from 1 to 4 carbon atoms, and the trifluoromethyl group, or (ii) A1 represents a straight- or branched-chain alkylene group containing from 1 to 10 carbon atoms and R1 represents a hydrogen atom, or a phenyl, phenoxy or phenylthio group each of which may optionally carry one or more substituents selected from halogen atoms, straight- or branched-chain alkyl or alkoxy groups, each containing from 1 to 4 carbon atoms, and the trifluoromethyl group, are new compounds of use in the field of mammalian reproduction and also of use in the control of insects and acarines.
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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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- Phosphonates containing protected ketone group
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The disclosure relates to novel protected ketone derivatives, for example dimethyl 3-(3-chlorophenoxy)-2-semicarbazonopropylphosphonate, for use as intermediates in the synthesis of known prostaglandin analogues, and to a process for their manufacture.
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