- ARYLMETHYLENE HETEROCYCLIC COMPOUNDS AS KV1.3 POTASSIUM SHAKER CHANNEL BLOCKERS
-
A compound of Formula (I) or a pharmaceutically acceptable salt thereof is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.
- -
-
Paragraph 0325; 0326
(2021/04/17)
-
- THERAPEUTIC METHODS
-
The invention provides methods and compositions for delivering a nucleic acid to a cell or the cytosol of the target cell. The method includes contacting the cell with, 1) a membrane-destabilizing polymer; and 2) a nucleic acid conjugate. The nucleic acid conjugate includes a targeting ligand bound to an optional linker and a nucleic acid.
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Page/Page column 135; 141-142
(2020/05/28)
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- H-Phosphonate Synthesis and Biological Evaluation of an Immunomodulatory Phosphoglycolipid from Thermophilic Bacteria
-
The synthesis of a library of bacterial phosphoglycolipid, PGL-1, is described. Key features of the synthesis include regioselective esterification of the primary alcohol of the diacylglycerol moiety and an H-phosphonate method to install the phosphate in PGL-1 in comparison with earlier reported procedures. A representative set of PGL-1 analogues was prepared and evaluated for their biological activities. Results showed that the immunological activity of PGL-1 is dependent on the chain lengths of the fatty acids.
- Gan, Chin Heng,Hua, Kuo-Feng,Lam, Yulin,Li, Lan-Hui,Peng, Yi-Jen,Wei, Chih-Feng,Wijaya, Hadhi,Wu, Shih-Hsiung
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supporting information
(2020/04/02)
-
- METHODS FOR TREATING HEPATITIS B INFECTIONS
-
Certain embodiments of the invention provide a method for identifying a patient that has a higher likelihood of responding to an HBV antigen inhibitor, such a method comprising detecting a hepatitis B virus (HBV) infected patient's genotype at one or more of the IL28B/A associated SNPs described herein, wherein the relevant genotype(s) described herein are indicative of a patient that has a higher likelihood of responding to an HBV antigen inhibitor as compared to an HBV infected patient having different genotypes at these locations.
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Page/Page column 209-210
(2019/04/09)
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- TARGETED COMPOSITIONS
-
The invention provides certain nucleic acids (e.g., double stranded siRNA molecules), as well as conjugates that comprise a targeting moiety, a double stranded siRNA, and optional linking groups. Certain embodiments also provide synthetic methods useful for preparing the conjugates. The conjugates are useful to target therapeutic double stranded siRNA to the liver and to treat liver diseases including hepatitis (e.g. hepatitis B and hepatitis D).
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Page/Page column 129; 130
(2018/11/10)
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- Electrochemical Oxidation of Alcohols and Aldehydes to Carboxylic Acids Catalyzed by 4-Acetamido-TEMPO: An Alternative to "anelli" and "pinnick" Oxidations
-
An electrocatalytic method has been developed to oxidize primary alcohols and aldehydes to the corresponding carboxylic acids using 4-acetamido-2,2,6,6-tetramethylpiperidin-1-oxyl (ACT) as a mediator. The method successfully converts benzylic, aliphatic, heterocyclic, and other heteroatom-containing substrates to the corresponding carboxylic acids in aqueous solution at room temperature. The mild conditions enable retention of stereochemistry adjacent to the site of oxidation, as demonstrated in a 40 g-scale synthesis of a precursor to levetiracetam, a medication used to treat epilepsy.
- Rafiee, Mohammad,Konz, Zachary M.,Graaf, Matthew D.,Koolman, Hannes F.,Stahl, Shannon S.
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p. 6738 - 6744
(2018/06/19)
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- [4-(1, 3, 3-TRIMETHYL-2-OXO-3, 4-DIHYDRO-1H-QUINOXALIN-7-YL) PHENOXY]ETHYLOXY COMPOUND OR SALT THEREOF
-
The present invention relates to a novel [4-(1,3,3-trimethyl-2-oxo-3,4-dihydro-1H-quinoxalin-7-yl)phenoxy]ethyloxy compound or a salt thereof. The compound or a salt thereof of the present invention has a glucocorticoid receptor agonist activity, and is u
- -
-
Paragraph 0123
(2018/07/29)
-
- TARGETED NUCLEIC ACID CONJUGATE COMPOSITIONS
-
The invention provides conjugates that comprise a targeting moiety, a nucleic acid, and optional linking groups as well as synthetic intermediates and synthetic methods useful for preparing the conjugates. The conjugates are useful to target therapeutic nucleic acids to the liver and to treat liver diseases including hepatitis (e.g. hepatitis B and hepatitis D).
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Page/Page column 102; 103
(2017/11/10)
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- SPIROCYCLIC HAT INHIBITORS AND METHODS FOR THEIR USE
-
Compounds having a structure of Formula (IX) or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b, R3a, R3b, R4a, R4b, Q1----Q2, R6, R7, A, B, W, x, and y are as defined herein and are provided. Pharmaceutical compositions comprising such compounds and methods for treating various HAT-related conditions or diseases, including cancer, by administration of such compounds are also provided.
- -
-
Page/Page column 711
(2016/04/10)
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- Synthesis of phospholipids on a glyceric acid scaffold: Design and preparation of phospholipase A2 specific substrates
-
Synthesis of a new series of phospholipid analogues to serve as activity-based probes of secretory phospholipase A2 enzymes is reported. The synthesis is based upon (1) preparation of long-chain esters and amides of glyceric acid, followed by (
- Rosseto, Renato,Hajdu, Joseph
-
p. 3155 - 3165
(2014/05/06)
-
- STEROL DERIVATIVES AND USE THEREOF FOR TREATING DISEASES INVOLVING TRANSFORMED ASTROCYTE CELLS OR FOR TREATING MALIGNANT HAEMOPATHIES
-
The invention relates to novel sterol derivatives, the preparation method thereof, pharmaceutical compositions containing them and use thereof for treating diseases involving transformed astrocyte cells or for treating malignant haemopathies. The inventio
- -
-
Page/Page column 25
(2013/12/03)
-
- Tetrapropylammonium perruthenate catalyzed glycol cleavage to carboxylic (Di)acids
-
A new method to accomplish glycol cleavage to carboxylic (di)acids in one step using catalytic amounts of tetrapropylammonium perruthenate (TPAP) together with N-methylmorpholine N-Oxide (NMO) as the stoichiometric oxidant is presented. In addition to regenerating the active catalyst, the N-oxide stabilizes intermediary carbonyl hydrates and thereby shifts a crucial equilibrium. The mild oxidation protocol is applicable to a broad range of substrates providing the respective acids, diacids, or keto acids in high yields.
- Schmidt, Andrea-Katharina C.,Stark, Christian B. W.
-
supporting information; experimental part
p. 5788 - 5791
(2011/12/05)
-
- Degradation of 1-deoxy-d-erythro-hexo-2,3-diulose in the presence of lysine leads to formation of carboxylic acid amides
-
A novel species of amides formed from degradation of one of the most important key intermediates in Maillard hexose chemistry-1-deoxyhexo-2,3- diulose-was investigated. In 1-deoxyhexo-2,3-diulose/Nα-t-BOC- lysine reaction mixtures four amides, Nε-acetyl lysine, N ε-formyl lysine, Nε-lactoyl lysine and N ε-glycerinyl lysine, were identified and their structures verified by authentic reference standards. Amides and corresponding carboxylic acids (acetic acid, formic acid, lactic acid and glyceric acid) accumulated over time. Both Nε-lysine amides and carboxylic acids were thus determined as stable Maillard end products. Results of model incubations suggested the synthesis of amides to be mechanistically closely related to the formation of their corresponding carboxylic acids by β-dicarbonyl cleavage. Due to the different chemical properties of all the compounds monitored, various analytical strategies had to be carried out (LC-MS2, GC-MS, GC-FID, enzymatic determination).
- Smuda, Mareen,Voigt, Michael,Glomb, Marcus A.
-
experimental part
p. 6458 - 6464
(2011/08/09)
-
- NOVEL COMPOUND 395
-
A compound of formula (1) and pharmaceutically acceptable salts thereof for use in the treatment of chemokine mediated diseases and conditions.
- -
-
Page/Page column 10
(2010/02/17)
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- Catalyzed dehydrogenative coupling of primary alcohols with water, methanol, or amines
-
A working partnership: Metal-ligand cooperativity is responsible for the high activity of the rhodium amido complex 1 in the dehydrogenative coupling of primary alcohols with water, methanol, or amines, including ammonia (see scheme), to give carboxylic acids, methyl carboxylates, or amides, respectively. The catalysis proceeds under mild reaction conditions in the presence of a recyclable hydrogen acceptor A. The multistep mechanism was elucidated by computational methods. (Chemical Equation Presented)
- Zweifel, Theo,Naubron, Jean-Valere,Gruetzmacher, Hansjoerg
-
supporting information; experimental part
p. 559 - 563
(2009/04/14)
-
- Studies on the synthesis of (-)-gymnodimine. Subunit synthesis and coupling
-
Two principal subunits of the marine algal toxin (-)-gymnodimine were synthesized. A trisubstituted tetrahydrofuran representing C10-C18 of the toxin was prepared via a highly stereoselective iodine-mediated cyclization of an acyclic alkene bearing a bis-
- White, James D.,Quaranta, Laura,Wang, Guoqiang
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p. 1717 - 1728
(2007/10/03)
-
- 8-Azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
-
The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
- -
-
Page/Page column 23
(2008/06/13)
-
- Synthetic studies towards 4,10-diaza-1,7-dioxaspiro[5.5]undecanes: access to 3-aza-6,8-dioxabicyclo[3.2.1]octan-2-one and 2H-1,4-oxazin-3(4H)-one frameworks
-
Synthetic approaches towards 4,10-diaza-1,7-dioxaspiro[5.5]undecanes starting from 1,3-dichloroacetone and solketal derivatives are explored. The method relies on the preparation of a key bis-substituted dihydroxy-protected oxime, which would undergo a final acidic deprotection-spiroacetalization process. Although the desired diazaspiroketal framework could not be obtained, our conditions led to the unexpected 3-aza-6,8-dioxabicyclo[3.2.1]octan-2-one 18 or to the oxazinone 32 in good yields.
- Goubert, Marlène,Toupet, Lo?c,Sinibaldi, Marie-Eve,Canet, Isabelle
-
p. 8255 - 8266
(2008/02/08)
-
- NOVEL TRIAZOLE COMPOUNDS AS ANTIBACTERIAL AGENTS AND THEIR PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
-
The present invention relates to novel triazole compounds of formula (I), where all symbols are as defined in the detailed description; their pharmaceutically acceptable salts their stereosiomers thereof, their prodrugs, their rotamers, their pharmaceutical compositions containing them. The present invention also relates to a process for the preparation of the above said novel compounds.
- -
-
Page/Page column 116
(2010/02/13)
-
- Method for producing carbonyl compound
-
[summary][PROBLEM TO BE SOLVED]: To provide a method for effectively producing carbonyl compound from alcohol using a ruthenium compound as an oxidation catalyst which can apply to various alcoholic compounds as starting materials, and to provide a method for effectively producing the carbonyl compound in high yield with decomposing neither the alcohol nor the produced carbonyl compound.[SOLUTION]: The method for producing carbonyl compound comprises the oxidative reaction process of alcohol using N-haloamide compound or N-haloimide compound in the presence of ruthenium compound of catalytic amount in the solvent containing organic solvent not substantially oxidized with the ruthenium compound The solvent used is solvent containing organic solvents other than the carboxylic acid; mixed solvent of pH5-14 containing organic solvent and water; or organic solvent containing base.
- -
-
Page/Page column 16-17; 22
(2008/06/13)
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- Solution-phase and solid-phase syntheses of enzyme inhibitor RK-682 and antibiotic agglomerins
-
The enzyme inhibitor RK-682 (5A)-(+)-1 was prepared in solution and on a solid support from (2R)-glycerates in five steps and ca. 40% overall yield. Key steps were a ring-closing tandem addition-Wittig alkenation reaction of the respective protected or im
- Schobert, Rainer,Jagusch, Garsten
-
p. 6129 - 6132
(2007/10/03)
-
- Synthetic studies of the cyclic depsipeptides bearing the 3-amino-6-hydroxy-2-piperidone (Ahp) unit. Total synthesis of the proposed structure of micropeptin T-20
-
The first total synthesis of a cyclic depsipeptide possessing the 3-amino-6-hydroxy-2-piperidone (Ahp) unit was successfully achieved in a convergent manner by the oxidative construction of the Ahp unit at the later stage of the synthesis. This synthetic work provides data indicating that the structure of the target Ahp-depsipeptide, micropeptin T-20, should be re-examined.
- Yokokawa, Fumiaki,Inaizumi, Akiko,Shioiri, Takayuki
-
p. 1459 - 1480
(2007/10/03)
-
- Synthesis and CB1 receptor activities of novel arachidonyl alcohol derivatives
-
Novel derivatives of arachidonyl alcohol were synthesized and evaluated for their CB1 receptor activity by [35S]GTPγS assay using rat cerebellar membranes.
- Parkkari, Teija,Savinainen, Juha R.,Rauhala, Anu L.,Tolonen, Tiina L.,Nevalainen, Tapio,Laitinen, Jarmo T.,Gynther, Jukka,Jaervinen, Tomi
-
p. 3231 - 3234
(2007/10/03)
-
- UREA-, GLYCERATE- AND, HYDROXYAMIDE-HEADED HYDROCARBON CHAIN LYOTROPIC PHASES FORMING SURFACTANTS
-
The invention provides a compound containing a head group based on urea, glycerol or glycerate and a tail selected from the group consisting of a branched alkyl chain, a branched alkyloxy chain or an alkenyl chain. The compounds may be used as surfactants to form a lyotropic phase that is stable in excess polar solution.
- -
-
-
- A practical RuCl3-catalyzed oxidation using trichlproisocyanuric acid as a stoichiometric oxidant under mild nonacidic conditions
-
The combined use of catalytic RuCl3 (1.0 mol %) and stoichiometric trichloroisocyanuric acid (TCCA; 1.0 equiv) in the presence of n-Bu4NBr (2.0 mol %) and K2CO3 (3.0 equiv) in 1:1 MeCN/H2O at 25-45°C allows smooth oxidation of primary alcohols to carboxylic acids. Secondary alcohols can be oxidized to ketones when using the same set of the reagents in 1:1 MeCN/ H2O or 1:1 AcOEt/H2O. By proceeding under the nonacidic biphasic conditions dispensing with hazardous reagents, the oxidation reactions are applicable to structurally diverse alcohols, easy to work up, environmentally benign, and basically high-yielding.
- Yamaoka, Hidenori,Moriya, Narimasa,Ikunaka, Masaya
-
p. 931 - 938
(2013/09/03)
-
- A new approach to the synthesis of lysophospholipids: Preparation of lysophosphatidic acid and lysophosphatidylcholine from p-nitrophenyl glycerate
-
A new stereospecific synthesis of lysophosphatidic acid and lysophosphatidylcholine is reported. The sequence relies on p-nitrophenyl-D- glycerate as a chiral synthon, including chemoselective reduction of the active ester function without affecting other carboxylic ester groups present in the molecule.
- Rosseto, Renato,Bibak, Niloufar,Hajdu, Joseph
-
p. 7371 - 7373
(2007/10/03)
-
- PROCESS FOR THE ENZYMATIC RESOLUTION OF 1,3-DIOXOLANE-4-CARBOXYLATES
-
The present invention relates to enzymatic' resolution of enantiomeric mixtures of 1,3-dioxolane-4-carboxylate esters of Formula I. More particularly, the present invention relates to a process for preparing R and S enantiomers of methyl 2,2-dimethyl-1,3-dioxolane-4-carboxylate in high optical purity.
- -
-
-
- Mapping the substrate selectivity of new hydrolases using colorimetric screening: Lipases from Bacillus thermocatenulatus and Ophiostoma piliferum, esterases from Pseudomonas fluorescens and Streptomyces diastatochromogenes
-
Recent advances in biochemistry and molecular biology have simplified the discovery and preparation of new hydrolases. Although these hydrolases might solve problems in organic synthesis, measuring their selectivity, especially enantioselectivity, remains tedious and time consuming. Recently, we developed a colorimetric screening method to measure the enantioselectivity of hydrolases. Here we apply this rapid screening method to map the substrate selectivity of four new hydrolases: lipases from the thermophilic Bacillus thermocatenulatus (DSM 730, BTL2) and a filamentous fungus Ophiostoma piliferum (NRRL 18917, OPL) and esterases from two bacteria, Pseudomonas fluorescens (SIK-W1, esterase I, PFE) and Streptomyces diastatochromogenes (Tue 20, SDE). We screened a general library of 29 substrates and a chiral library of 23 pairs of enantiomers. All four hydrolases catalysed the hydrolysis of unnatural substrates, but the two lipases accepted a broader range of substrates than the two esterases. As expected, the two lipases favoured more hydrophobic substrates, while the two esterases showed a preference for smaller substrates. Several moderately enantioselective reactions were identified for the solketal esters: BTL2, butyrate, E = 7.9 (R); octanoate, E = 4.9 (R) and 3-bromo-2-methyl propionate methyl esters, PFE, E = 12 (S); SDE, E = 5.6 (S). OPL showed low enantioselectivity toward all substrates tested. The current colorimetric screen could not measure the selectivity for several slow-reacting substrates. Traditional screening identified high enantioselectivity of BTL2 and PFE toward one of these slow substrates, 1-phenylethyl acetate (E>50).
- Liu, Andrew Man Fai,Somers, Neil A.,Kazlauskas, Romas J.,Brush, Terry S.,Zocher, Frank,Enzelberger, Markus M.,Bornscheuer, Uwe T.,Horsman, Geoff P.,Mezzetti, Alessandra,Schmidt-Dannert, Claudia,Schmid, Rolf D.
-
p. 545 - 556
(2007/10/03)
-
- Thienopyridine compounds, their production and use
-
The compound of the present invention possesses excellent gonadotropin-releasing hormone antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases, e.g., sex hormone-dependent cancers (e.g., prostatic cancer, uterine cancer, breast cancer, pituitary tumor), prostatic hypertrophy, hysteromyoma, endometriosis, precocious puberty, amenorrhea syndrome, multilocular ovary syndrome, pimples etc, or as a pregnancy regulator (e.g., contraceptive), infertility remedy or menstruation regulator.
- -
-
-
- Asymmetric synthesis of (2'R,4'R) and (2'S,4'S)-1,3-dioxolanyl triazole C-nucleosides
-
In view of biological activities of both 1,3-dioxolanyl nucleosides and C-nucleosides, D- and L-1,3-dioxolanyl C-nucleosides have been synthesized as potential antiviral and/or anticancer agents. Asymmetric synthesis of four new optically pure D- and L-1,
- Qu, Fucheng,Hong, Joon H.,Du, Jinfa,Newton, M. Gary,Chu, Chung K.
-
p. 9073 - 9088
(2007/10/03)
-
- General solid-phase synthesis approach to prepare mechanism-based aspartyl protease inhibitor libraries. Identification of potent cathepsin D inhibitors
-
A general method has been developed for the expedient solid-phase synthesis of aspartyl protease inhibitors that do not incorporate any amino acids. The synthesis approach was designed to allow the introduction of diverse functionality at all four variabl
- Lee, Christina E.,Kick, Ellen K.,Ellman, Jonathan A.
-
p. 9735 - 9747
(2007/10/03)
-
- Investigation of glycerol incorporation into soraphen A
-
Glycerol has been incorporated mid-chain into the polyketide soraphen A 1 at C-3,4 and C-11,12; the pro-(S)-hydroxymethyl group of glycerol is lost and one of the hydrogens in the pro-(R)-hydroxymethyl group is retained at C-11 which excludes hydroxymalonate as the immediate precursor to the vicinal methoxy groups at C-11,12.
- Hill, Alison M.,Harris, Jonathan P.,Siskos, Alexandros P.
-
p. 2361 - 2362
(2007/10/03)
-
- 1,3-dioxolane C-nucleosides: Asymmetric synthesis of four stereoisomers of 2-[2-(hydroxymethyl)-1,3-dioxolan-5-yl]-1,3-thiazole-4-carboxamide
-
Asymmetric synthesis of four novel C-nucleosides, (2′R,5′R)-, (2′S,5′R)-, (2′S,5′S)- and (2′R,5′S)-2-[2-hydroxymethyl)-1,3-dioxolan-5-yl]-1,3-thiazole-4- carboxamide has been accomplished by the condensation of key intermediates, 2-(1R- and 1S-glycol-1-yl)-4-ethoxycarbonyl-1,3-thiazole with 2-benzoyloxy acetaldehyde dimethyl acetal.
- Jinfa, Du,Fucheng, Qu,Lee Doo-won,Gary Newton,Chu Chung
-
p. 8167 - 8170
(2007/10/02)
-
- A route to homochiral (S)-O-methyl mandelic acid and related α-alkoxy carboxylic acids from isopropylidene glycerol
-
An improved synthesis of the useful ketones 7 is described. These ketones are then further modified via a highly stereospecific reduction to give homochiral α-alkoxy carboxylic acids which are useful chiral auxiliaries and intermediates.
- Handa,Hawes,Pryce
-
p. 2837 - 2845
(2007/10/02)
-
- Scope and Mechanism of Deprotection of Carboxylic Esters by Bis(tributyltin) Oxide
-
Methyl and ethyl esters of aliphatic and aromatic carboxylic acids as well as benzyl carboxylates, thiol esters and double esters such as (pivaloyloxy)methyl carboxylates have been successfully cleaved with bis(tributyltin) oxide to give the free carboxylic acids in good yields.The reaction is carried out in aprotic solvents under essentially neutral conditions and thus this method can serve as an ideal procedure for the cleavages of esters with other functional groups and/or protecting groups acid and/or base sensitive.We demonstrated that the reaction displays a high level of chemoselectivity between methyl and ethyl esters versus tert-butyl esters and γ-lactones.Bis(tributyltin) oxide is also a highly efficient reagent for the cleavage of acetates of primary and secondary alcohols and phenols.The limitations we found in the use of this reagent include the lack of cleavage of esters sterically hindered around the carboxyl carbon and the carbinol group (i.e., esters of tertiary alcohols) and in carboxylic esters that contain a fluoroalkyl substituent.A resonable mechanistic explanation is discussed to account for the reaction pathway of the acyloxygen cleavage of (-)-(1R)-menthyl acetate.
- Salomon, Claudio J.,Mata, Ernesto G.,Mascaretti, Oreste A.
-
p. 7259 - 7266
(2007/10/02)
-
- Enzymes in Organic Synthesis, 15. Synthesis of Methyl (S)-(-)-2,3-O-Isopropylideneglycerate by Enantioselective Enzyme-Catalyzed Hydrolysis of Methyl (+/-)-2,3-O-Isopropylideneglycerate
-
In contrast to porcine pancreatic lipase (PPL), the serine proteases aP 41 and thermitase are suited as catalysts for the enantioselective ester hydrolysis of methyl (+/-)-2,3-O-isopropylideneglycerate (rac-1).These enzymes allow the preparation of methyl (S)-(-)-2,3-O-isopropylideneglycerate (1) with an enantiomeric excess of 84-87percent in a yield of 19-27percent related to the starting racemate. Key Words: Enzymes / Proteases / Ester hydrolysis, enzymatic / Isopropylideneglycerates / Resolution, kinetic / Glycerates
- Schick, Hans,Schroetter, Eberhard,Szymanowski, Matthias,Knoll, Alexander
-
p. 103 - 104
(2007/10/02)
-
- Process for preparing 1,3-dioxolane ketones
-
A process for preparing a ketone of the general formula: STR1 in which R1 and R2 each independently represent a C1-6 alkyl or C6-12 aryl group, and R represents an alkyl, aryl, aralkyl, heterocyclic or carboxyli
- -
-
-
- Oxidation of partially protected carbohydrates at the nickel hydroxide electrode
-
Primary hydroxy groups in pyranoses are oxidized in excellent yields to the corresponding carboxylic acids. In furanose 3 the yield of acid is only moderate. Secondary hydroxy groups are inert, aside from lactols. The different reactivity of secondary and primary hydroxy groups allows the chemoselective oxidation of 8 and 10.
- Schaefer, Hans J.,Schneider, Roy
-
p. 715 - 724
(2007/10/02)
-
- Synthesis of chiral and achiral pyranenamine derivatives. Potent agents with topical ocular antiallergic activity
-
The SS, RR and meso stereoisomers of pyranenamine SK and F 84210 (2) were synthesized stereospecifically starting from commercially available (R)-(-)- or (S)-(+)-2,2-dimethyl-1,3-dioxolane-4-methanol (3). In addition, two achiral pyranenamines 19 and 26 w
- Gluchowski,Bischoff,Garst,Kaplan,Dietrich,Aswad,Gaffney,Aoki,Garcia,Wheeler
-
p. 392 - 397
(2007/10/02)
-
- ENZYMATIC ENANTIOSELECTIVE HYDROLYSIS OF 2,2-DIMETHYL-1,3-DIOXOLANE-4-CARBOXYLIC ESTERS
-
2,2-dimethyl-1,3-dioxolane-4-carboxylic acid derived chiral building blocks were prepared from substituted α,β-unsaturated acids with high enantiomeric purities by enzymatic hydrolysis of their n.butyl esters.
- Pottie, M.,Eycken, J. Van der,Vandewalle, M.,Dewanckele, J. M.,Roeper, H.
-
p. 5319 - 5322
(2007/10/02)
-
- D-GLYCOPYRANOSYL PHENYLSULPHONES: ACYLATION OF THEIR LITHIATED ANIONS AND REDUCTIVE DESULFONYLATION OF THE RESULTING ACYLATED SULFONES. A SYNTHESIS OF α-D-GLYCOSIDES
-
The lithiated anion of 3,4,6-tri-O-t-butyldimethylsilyl-2-deoxy-α,β-D-glucopyranosyl phenylsulfone reacts with dimethylcarbonate and various phenyl esters to give stable acylated products.Subsequent reductive lithiation leads to enolates which ungergo kin
- Beau, Jean-Marie,Sinay, Pierre
-
p. 6193 - 6196
(2007/10/02)
-