- ENANTIOMERIC RESOLUTION OF 2,4-DISUBSTITUTED 1,3-OXATHIOLANE NUCLEOSIDES
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Single enantionmers of compounds of formula (B), in either the cis or trans configuration, wherein R1 and R2 are as defined herein, can be separated from enantiomeric mixtures thereof by reacting the compound with an acid to produce
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- A PROCESS FOR CHIRAL RESOLUTION OF 2-SUBSTITUTED 4-SUBSTITUTED 1,3-OXATHIOLANES
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The present invention relates to a novel process for the chiral resolution of 2-substituted 4-substituted 1,3-oxathiolanes and derivatives thereof. The present invention also relates to novel 2-substituted 4-substituted 1,3-oxathiolanes derivatives.
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Page/Page column 69-70
(2009/05/29)
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- Enantiomeric resolution of 2-substituted 4-substituted 1,3-oxathiolanes nucleosides
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Single enantionmers of compounds of formula (B), in either the cis or trans configuration, wherein R1 and R2 are as defined herein, can be separated from enantiomeric mixtures thereof by reacting the compound with an acid to produce a conglomerate salt that has the following characteristics: the IR spectrum of the salt of the racemic compound, a 1:1 mixture of (?) and (+) crystals, is identical to that of the each of the single enantiomer, andthe salt of the racemic compound has a melting point lower that that of either single enantiomer. The conglomerate salt is then separated by preferential crystallization.
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Page/Page column 11
(2009/04/24)
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- PROCESS AND METHODS FOR THE PREPARATION OF OPTICALLY ACTIVE CIS-2-HYDROXYMETHYL-4-(CYTOSIN-1′-YL)-1,3-OXATHIOLANE OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
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There is provided a method for resolving a compound of formula (III), in the cis configuration: There is also provided a process for producing optically active compound of formula (I) or (II): wherein: R1, R2, R3 are as de
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Page/Page column 26
(2008/06/13)
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- Process and methods for the preparation of optically active cis-2-hydroxymethyl-4- (cytosin-1'-yl) -1,3-oxathiolane or pharmaceutically acceptable salts thereof
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There is provided a method for resolving a compound of formula III, in the cis configuration: There is also provided a process for producing optically active compound of formula I or II: wherein: R1, R2, R3 are as defined
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Page/Page column 10
(2008/06/13)
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- Substituted 1,3-oxathiolanes with antiviral properties
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This invention relates to single enantiomers of novel cis-substituted 1,3-oxathiolanes, of the formula (I): wherein; R1is hydrogen, and R2is cytosine or 5-fluorocytosine; and pharmaceutically acceptable salts and esters thereof. This invention also relates to pharmaceutical compositions containing them and to the use of these compounds as antiviral agents, particularly in combination therapy.
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- Substituted 1,3-oxathiolanes with antiviral properties
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This invention relates to single enantiomers of novel cis-substituted 1,3-oxathiolanes, of the formula (I): wherein; R1is hydrogen, and R2is cytosine or 5-fluorocytosine, and pharmaceutically acceptable salts and esters thereof. This
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- A new strategy for the asymmetric synthesis of 1,3-oxathiolane-based nucleoside analogues
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A ready asymmetric synthesis of 3'-oxathionucleosides has been accomplished in three main steps from benzoyloxyethanal. The synthesis is characterized by high overall yield and considerable enantiomeric excesses. It represents a general synthetic path to prepare a wide range of heterosubstituted sulfur-containing nucleoside analogues.
- Caputo, Romualdo,Guaragna, Annalisa,Palumbo, Giovanni,Pedatella, Silvana
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p. 1455 - 1458
(2007/10/03)
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- Short synthesis of 2,4-disubstituted 1,3-oxathiolane and 1,3-dithiolane cytosine nucleosides: Facile introduction of a 4-benzoate group using benzoyl peroxide
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Introduction of a benzoate group at position 4 in 2-substituted 1,3- oxathiolane and 1,3-dithiolane using benzoyl peroxide is described. The coupling reaction between 1,3-oxathiolane derivatives 3 and pyrimidine bases in the presence of TMSI produced cis
- Nguyen-Ba, Nghe,Brown, William,Lee, Nola,Zacharie, Boulos
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p. 759 - 762
(2007/10/03)
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- Substituted 1,3-oxathiolanes and substituted 1,3-dithiolanes with antiviral properties
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This invention relates to novel substituted 1,3-oxathiolanes and substituted 1,3-dithiolanes or pharmaceutically acceptable salts and esters thereof, of the formula: STR1 wherein X is S, S=O, or SO2 ; Y is O, S, S=O, or SO2 ; R1
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- Structure-activity relationships among a new class of antiviral heterosubstituted 2',3'-dideoxynucleoside analogues
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3'-Oxa-4'-thiocytidine nucleoside analogues 14-17 were prepared from oxathiolanes 10 and 11, and evaluated for activity against HIV-1 and HBV in vitro. The nucleoside analogues were found to possess potent activities against HIV-1 in a panel of cell lines. Compound 16 is moderately active against HBV in 2.2.15 cells.
- Mansour,Jin,Wang,Dixit,Evans,Tse,Belleau,Gillard,Hooker,Ashman,Cammack,Salomon,Belmonte,Wainberg
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p. 627 - 635
(2007/10/02)
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- Synthesis of Optically Active 2',3'-Dideoxy-3'-oxa-4'-thio-ribonucleoside Analogues by Transposition of a Leaving Group on Chiral Oxathiolanes via a Reductive-oxidative Process
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The synthesis of chiral nucleoside analogues with a unique structural feature is reported.The strategy is based on a reductive-oxidative process to complete the transposition of the leaving group in chiral oxathiolanes with known configuration.
- Wang, Wei,Jin, Haolun,Mansour, Tarek S.
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p. 4739 - 4742
(2007/10/02)
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