- POLY(PHOSPHOESTERS) FOR DELIVERY OF NUCLEIC ACIDS
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Disclosed are polymers comprising the moiety A, which is a moiety of formula I: and pharmaceutically acceptable salts thereof, wherein R, R1, R2, L, n1 and n2 are as defined herein. These polymers are useful for delivering nucleic acids to subject. These polymers and pharmaceutically acceptable compositions comprising such polymers and nucleic acids can be useful for treating various diseases, disorders and conditions.
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- Design and preparation of a novel prolinamide-based organocatalyst for the solvent-free asymmetric aldol reaction
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The preparation of four novel organocatalysts as highly diastereo and enantioselective catalysts for the solvent-free asymmetric aldol reaction was described. These organocatalysts were synthesized in eight steps applying simple and commercially available starting materials. The best results were obtained for the proline-derived catalyst, providing access to the desired adducts in up to 95% yield, 1:19 syn/anti and 98% e.e. Moreover, even sterically bulky aldehydes and substituted cyclohexanones were well tolerated. DFT calculations and control experiments indicated that several hydrogen bonding interactions between the aldehyde and the enamine intermediate are responsible for the stereoselective chiral induction process and that the trifluoroacetate counter-anion is crucial for the attainment of higher stereoselectivities.
- Martins, Rafaela de S.,Pereira, Mathias P.,de Castro, Pedro P.,Bombonato, Fernanda I.
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supporting information
(2019/12/24)
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- PROCESS FOR PREPARING SOLKETAL AMINE VIA DIRECT AMINATION
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Disclosed a process for preparing a solketal amine via direct amination. It is possible to obtain solketal amines by very simple procedure with desired characteristics such as simplicity, inexpensiveness, high yield and conversion, as well as low environmental impact.
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Page/Page column 15
(2020/03/23)
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- PROCESS FOR THE PREPARATION OF A 3-AMINO-1,2-PROPANDIOL AND DERIVATIVES THEREOF
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Process for the preparation of a compound of formula (I) with R1 and R2 independently from each other representing hydrogen or a C1-to C10 alkyl group by a two-step process wherein the first step is an amination of the compound of formula (II) with an amino compound HNR1 R2 in the presence of hydrogen and resulting in the compound of formula (III) and the second step is a ring-cleaving of the compound of formula (III) giving the compound of formula (I).
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Page/Page column 9
(2019/02/13)
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- Chemo- and Site-Selective Alkyl and Aryl Azide Reductions with Heterogeneous Nanoparticle Catalysts
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Site-selective modification of bioactive natural products is an effective approach to generating new leads for drug discovery. Herein, we show that heterogeneous nanoparticle catalysts enable site-selective monoreduction of polyazide substrates for the generation of aminoglycoside antibiotic derivatives. The nanoparticle catalysts are highly chemoselective for reduction of alkyl and aryl azides under mild conditions and in the presence of a variety of easily reduced functional groups. High regioselectivity for monoazide reduction is shown to favor reduction of the least sterically hindered azide. We hypothesize that the observed selectivity is derived from the greater ability of less-hindered azide groups to interact with the surface of the nanoparticle catalyst. These results are complementary to previous Staudinger reduction methods that report a preference for selective reduction of electronically activated azides.
- Udumula, Venkatareddy,Nazari, S. Hadi,Burt, Scott R.,Alfindee, Madher N.,Michaelis, David J.
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p. 4423 - 4427
(2016/07/12)
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- AMINOPYRIMIDINONES AS INTERLEUKIN RECEPTOR-ASSOCIATED KINASE INHIBITORS
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This invention relates to aminopyrimidinone compounds of Formula (I) that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment or prevention of inflammatory diseases, including rheumatoid arthritis and inflammatory bowel disease.
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Page/Page column 169; 170
(2013/05/22)
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- 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
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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
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p. 8255 - 8266
(2008/02/08)
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- 2-aminopyridine derivatives and combinatorial libraries thereof
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The present invention relates to novel 2-aminopyridine derivative compounds of the following formula: wherein R1to R5have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing 2-aminopyridine derivative compounds.
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- Efficient Pathways to (R)- and (S)-5-Hydroxymethyl-2-oxazolidinone and some Derivatives
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2-Oxazolidinones are a very interesting class of compounds due to their various pharmacological effects.Two new syntheses of enantiomerically pure (R)- and (S)-5-hydroxymethyl-2-oxazolidinone have been developed starting with D-mannitol, L-ascorbic acid and (R)- or (S)-malic acid. (R)- and (S)-5-hydroxymethyl-2-oxazolidinone have been used to synthesize some new homochiral 2-oxazolidinone derivatives.
- Danielmeier, Karsten,Steckhan, Eberhard
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p. 1181 - 1190
(2007/10/02)
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