- Synthesis of new heteroleptic strontium complexes
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A series of heteroleptic strontium complexes (1-9) using a combination of different aminoalkoxides and 2,2,6,6-tetramethyl-3,5-heptanedionate (tmhd) were prepared to examine the effect of the bulkiness and coordination ability of the aminoalkoxide ligand in these complexes as well as potential strontium precursors. All complexes were characterized by FT-IR, FT-NMR, elemental analyses, and thermo-gravimetric (TG) analyses. The crystal structure analyses of 1, 2, 4, and 5 demonstrate their stability in the dimer form and the unwillingness of the strontium atom to form more than six coordination bonds in these complexes. The complex 5 shows an unusual picture: the existence of one hexa-coordinated and one penta-coordinated strontium atom side by side in its dimer structure. The introduction of ether groups as coordination sites in complexes 6-9 led to a decrease in steric hindrance which resulted in the formation of the complex 7 as a tetramer. The complex 7 shows a unique Sr4O4cubane core where oxygen atoms undergo μ3-bridging between strontium atoms. The TG analyses show that the complexes exhibit a step-wise decomposition character, with the major mass losses in the region 150-400 °C.
- George, Sheby Mary,Kim, Hyo-Suk,Park, Bo Keun,Kim, Chang Gyoun,Chung, Taek-Mo,Lah, Myoung Soo
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Read Online
- Preparation method of escitalopram oxalate impurities
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The application of the invention provides a brand-new preparation method of (R)-4-(dimethylamino)-1-(1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-yl)-butyl-1-ketone to provide a basis for qualitative and quantitative analysis of impurity profiles in escitalopram oxalate finished products, thereby having a significant role in quality control of escitalopram oxalate and being capable of promoting the safe use of depressive patients.
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Paragraph 0022
(2017/08/29)
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- SELECTIVE ALLOSTERIC MODULATORS OF THE SEROTONIN TRANSPORTER
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Compounds of formula (I) are provided wherein R1 represents H, CN and CF3; R2 represents 1-naphthyl, 3,5-dichlorophenyl, 4-(4-fluorophenylthio)phenyl or phenyl substituted with one or more substituent selected from halogen, methoxy, cyano, methyl and trifluorom ethyl; R3 and R4 independently represent H, C1-3-alkyl or R3 and R4 together with the carbon atom to which they are attached form a C4-6-cyclic alkyl; R5 and R6 independently represent H or C1-6-alkyl; n represents 1 or 2; and pharmaceutically acceptable acid addition salts thereof, provided that if n is 2 then R2 is not 1-naphthyl, which compounds are selective allosteric SERT ligands.
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Page/Page column 26
(2013/08/15)
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- NOVEL PHTHALOCYANINE DERIVATIVES FOR THERAPEUTIC USE
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There are described phthalocyanine derivates, the pharmaceutical compositions and the medical devices that contain them, possibly in combination with chelating agents, such as EDTA, useful for treating, by means of photodynamic therapy, diseases character
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Page/Page column 10; 11
(2013/03/26)
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- Preparation of Escitalopram, Its Salts and Intermediates
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The present patent application relates to an improved process for the preparation of escitalopram, its salts and intermediates. It also relates to a novel crystalline form S of citalopram diol intermediate, process for preparation and its use in the preparation of citalopram, escitalopram and their salts.
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Page/Page column 6
(2011/05/03)
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- PREPARATION OF ESCITALOPRAM, ITS SALTS AND INTERMEDIATES
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The present patent application relates to an improved process for the preparation of escitalopram, its salts and intermediates. It also relates to a novel crystalline form S of citalopram diol intermediate, process for preparation and its use in the preparation of citalopram, escitalopram and their salts.
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Page/Page column 16-17
(2010/04/03)
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- From the selective serotonin transporter inhibitor citalopram to the selective norepinephrine transporter inhibitor talopram: Synthesis and structure-activity relationship studies
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Citalopram and talopram are structurally closely related, but they have very distinct pharmacological profiles as selective inhibitors of the serotonin and norepinephrine transporters, respectively. A systematic structure-activity relationship study was p
- Eildal, Jonas N. N.,Andersen, Jacob,Kristensen, Anders S.,J?rgensen, Anne Marie,Bang-Andersen, Benny,J?rgensen, Morten,Str?mgaard, Kristian
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scheme or table
p. 3045 - 3048
(2009/04/05)
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- Method for the preparation of citalopram
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A method for the preparation of citalopram and its pharmaceutically acceptable salts is described; it's obtained starting from 5-cyanophthalide by reaction with a mixture of 4-fluorophenyl magnesium bromide and 3-dimethylaminopropyl magnesium chloride. The intermediate obtained is showed here-below: wherein X is an halogen, preferably chlorine or bromine, which is cyclized without any isolation.
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Page/Page column 5
(2008/06/13)
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- IMPROVED PROCESS FOR THE MANUFACTURE OF CITALOPRAM HYDROBROMIDE
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The present invention describes an improved process for the preparation of extremely pure 1-(4'-Fluorophenyl)-1-(3-dimethylaminopropyl)-5-phthalanecarbonitrile and its bromide salt (citalopram hydrobromide), which is a well known antidepressant. Other aspect of the invention are isolation of crystalline (4-Bromo-2-hydroxymethyl)phenyl-(4-fluorophenyl)-3-(dimethylaminopropyl)methanol (Bromodiol) and conversion of desmethylcitalopram which is formed during the cyanide exchange reaction, to Citalopram by heating with a mixture of formaldhyde and formic acid in chloroform. The resulting citalopram is conventionally purified using extraction methodology.
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Page/Page column 9-10
(2008/06/13)
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- ONE POT SYNTHESIS OF CITALOPRAM FROM 5-CYANOPHTHALIDE
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A process for one pot synthesis of citalopram is disclosed. The process comprises subjecting 5-cyano phthalide to Grignard reduction followed cyclization and followed by C-alkylation reaction to obtain citalopram without isolation and purification of any intermediates. In another embodiment, 5-cyano phthalide is subjected to sequential Grignard reactions followed by cyclization to obtain citalopram without isolation and purification of any intermediate stages.
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Page/Page column 10-11
(2008/06/13)
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- Method of manufacturing citalopram
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The present invention provides, inter alia, a novel process for the preparation of Citalopram, a known antidepressant.
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Page/Page column 24
(2010/02/11)
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- Process for the preparation of citalopram
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Preparation of citalopram comprises the steps of: (a) converting the compound of Formula (I) to a compound of Formula (II), wherein R in Formula (I) represents a C2 to C5 alkylene group which may be substituted or unsubstituted, and R1 in the compounds of Formula (II) represents a carboxylic acid group or a salt or an ester thereof; and (b) converting the compound of Formula (II) to form citalopram or a pharmaceutically acceptable salt thereof, or a direct conversion of the compound of Formula (I) to citalopram
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- PROCESS AND INTERMEDIATES FOR PREPARING ESCITALOPRAM
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The antidepressant drug Escitalopram is prepared from 5-bromophthalide via the diol intermediate (4-bromo-2-(hydroxymethyl)phenyl)-(4-fluorophenyl)methanol. The racemic diol intermediate is converted to an enantiomerically enriched form by first converting the diol to a monoester intermediate and then reacting the monoester intermediate with an optically active acid, most preferably (+)-di-p-toluoyl tartaric acid, to form a salt. The salt is then crystallized to recover an enantiomerically enriched, crystalline form thereof. The monoester intermediate is preferably formed by reacting the racemic diol intermediate with an acid or a reactive acid derivative which, in a particularly preferred embodiment, is acetic anhydride.
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Page/Page column 9-10
(2008/06/13)
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- DIBENZ[B,E]OXEPIN DERIVATIVE AND PHARMACEUTICAL COMPOSITIONS THEREOF
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Novel dibenz[b,e]oxepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma and also employed in the treatment of inflammation.
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- 2-Oxo-3-alkenyl dimethylamine
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(2-oxo-3-butenyl)dimethylamine monomers which may be used in the preparation of high molecular weight water-soluble cationic polymers which may be used as flocculants, drainage and retention aids, or conductive polymers.
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- Alkenyl- and alkanylamines
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Novel alkenyl- and alkanylamines having the formula: EQU1 WHEREIN Am is lower-alkylamino, di-lower-alkylamino and piperidino; A is methylene and methylidyne; R is hydrogen, lower-alkyl, lower-alkoxy, halogen and trifluoromethyl; m is zero and one; n is one and two; X is halogen and the pharmaceutically acceptable acid addition salts thereof. The alkenylamines are prepared by contacting 1-cyclopropyl-1-phenyl-ω-amino-1-alkanols with strong mineral acids. The alkanylamines are prepared by hydrogenation of the alkenylamines. Some of the compounds exhibit potent antagonism to the depressant effects of tetrabenazine.
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- 10,11-Dihydro-5-(3-amino-propyl-or-propylidene)-10,10,11,11-tetra-fluoro-5H-dibenzo[a,d]cycloheptenes and-5-ols
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Tetrafluoro derivatives of 10,11-dihydro-5H-dibenzo[a,d]cycloheptene-5-propylamine and 10,11-dihydro-5H-dibenzo[a,d]cycloheptene-Δ-5-γ-propylamine, useful as antidepressants, are prepared from the known 10,11-dihydro-5H-dibenzo[a,d]cycloheptene-10,11-dione by fluorination at the 10,11- position using sulfur tetrafluoride followed by introduction of the amino propylidine or the amino propyl substituent at the 5- position by reaction of the 5-keto or 5-halo-10,10,11,11-tetrafluoro derivative with the appropriate Grignard reagent.
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