- Organocatalytic Enantioselective Addition of α-Aminoalkyl Radicals to Isoquinolines
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With a dual organocatalytic system involving a chiral phosphoric acid and a dicyanopyrazine-derived chromophore (DPZ) photosensitizer and under the irradiation with visible light, an enantioselective Minisci-type addition of α-amino acid-derived redox-active esters (RAEs) to isoquinolines has been developed. A variety of prochiral α-aminoalkyl radicals generated from RAEs were successfully introduced on isoquinolines, providing a range of valuable α-isoquinoline-substituted chiral secondary amines in high yields with good to excellent enantioselectivities.
- Liu, Xiangyuan,Liu, Yang,Chai, Guobi,Qiao, Baokun,Zhao, Xiaowei,Jiang, Zhiyong
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supporting information
p. 6298 - 6301
(2018/10/09)
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- Preparation method of O-methyl-threonine/tyrosine
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The invention relates to a preparation method of O-methyl-threonine/tyrosine. The preparation method mainly overcomes the disadvantages of the existing method that a toxic reagent is volatile, the reagent is dangerous, the steps are long, the yield is low, and the like. The preparation method of the O-methyl-threonine/tyrosine comprises the following steps: N-t-butyloxycarboryl-threonine/tyrosineis catalyzed by sodium hydroxide and reacts with dimethyl sulfate to generate N-t-butyloxycarboryl-O-methyl-threonine/tyrosine, and then t-butyloxycarboryl is removed from the N-t-butyloxycarboryl-O-methyl-threonine/tyrosine through acid substances to obtain the product O-methyl-threonine/tyrosine. The product has important application in the fields of antibiotics and polypeptide drugs.
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Paragraph 0017
(2018/06/21)
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- Immunomodulatory peptides
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The invention relates to peptides derivatized with a hydrophilic polymer which, in some embodiments, bind to human FcRn and inhibit binding of the Fc portion of an IgG to an FcRn, thereby modulating serum IgG levels. The disclosed compositions and methods may be used in some embodiments, for example, in treating autoimmune diseases and inflammatory disorders. The invention also relates, in further embodiments, to methods of using and methods of making the peptides of the invention.
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- Enhanced reduction of C-N multiple bonds using sodium borohydride and an amorphous nickel catalyst
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Amorphous nickel powder (Ni0) was utilised as a catalyst under mild, aqueous, basic conditions for enhancing the sodium borohydride-mediated reduction of C-N multiple bonds such as oximes, imines, hydrazones and nitriles to produce the corresponding amines in good to excellent yields.
- Liu, Shouxin,Yang, Yihua,Zhen, Xiaoli,Li, Junzhang,He, Huimin,Feng, Juan,Whiting, Andrew
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experimental part
p. 663 - 670
(2012/01/15)
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- [B]-FUSED BICYCLIC PROLINE DERIVATIVES AND THEIR USE FOR TREATING ARTHRITIC CONDITIONS
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The invention relates to a compound which is [b]-fused bicyclic proline derivative, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition comprising the compound or the salt thereof, and methods of treating diseases, including, but not limited to, methods of preventing or inhibiting joint cartilage damage and preventing or treating diseases characterized by joint cartilage damage, joint inflammation, or joint pain. The [b]-fused bicyclic proline derivatives are compounds of Formula I as described above. Diseases characterized by joint cartilage damage or joint pain include, for example, osteoarthritis and rheumatoid arthritis. Rheumatoid arthritis is also characterized by joint inflammation. This invention also relates to methods of synthesizing and preparing the [b]-fused bicyclic proline derivatives, or a pharmaceutically acceptable salt thereof.
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- Solid phase reduction of oxazolones using BER-Ni2B-A simple synthesis of N-benzoylphenylalanines
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Borohydride exchange resin (BER)-Ni2B is successfully used as a reagent for the solid phase reduction of the C-4 exocyclic double bond of oxazolones to give the N-benzoylphenylalanines and hence the corresponding amino acids.
- Sikdar, Atul P.,Chetri, Ajoy B.,Das, Pranab J.
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p. 2878 - 2881
(2007/10/03)
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- Substituted quinoxaline-2-ones as glutamate receptor antagonists
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A novel series of substituted quinoxaline 2-ones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the compounds are also taught. The compounds are glutamate receptor antagonists and are useful in the treatment of stroke, cerebral ischemia, or cerebral infarction resulting from thromboembolic or hemorrhagic stroke, cerebral vasospasms, hypoglycemia, cardiac arrest, status epilepticus, perinatal asphyxia, anoxia, seizure disorders, pain, Alzheimer's, Parkinson's, and Huntington's Diseases.
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- α-Isocyanatoacrylonitriles from alkylidene- or arylidenecyanoacetic acids; synthesis and reactions
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The Curtius reaction converts alkylidene- or arylidenecyanoacetic acids to α-isocyanatoacrylonitriles in a stereospecific way. These versatile intermediates allow an easy access to arylacetic acids and various amino acid derivatives, as well as β-lactams or 2-azabutadienes.
- Jaafar,Francis,Danion-Bougot,Danion
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- SOLID-LIQUID PHASE TRANSFER CATALYTIC SYNTHESIS OF α-AMINO ACID VIA ALKYLATION AND NUCLEOPHILIC ADDITION OF BENZALDEHYDE IMINES
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A short, mild and efficient synthetic route of α-amino acid via alkylation, Michael addition and carbonyl addition as well as cycloaddition of aldimines derived from glycine and alanine esters with benzaldehyde under solid-liquid phase transfer catalytic condition has been studied.The key to solid-liquid phase transfer catalyzed reactions is the selection of a base for the various reactants.The yield is dependent on the base used.The results obtained using KOH, K2CO3 and Na2CO3 are discussed.The kinetics of solid-liquid PTC benzylation has been investigated and we propose a possible mechanism of solid-liquid PTC as an interface auto-catalytic procedure.The details of some syntheses of α-amino acids are presented.
- Yaozhong, Jiang,Changyou, Zhou,Shengde, Wu,Daimo, Chen,Youan, Ma,Guilan, Liu
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p. 5343 - 5354
(2007/10/02)
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- Tetrahydrofurnancarboxylic acid derivatives, processes for preparation thereof and pharmaceutical compositions thereof
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This invention relates to tetrahydrofuran-carboxylic acid derivatives, of antimicrobial activity, of the formula: STR1 wherein R1 is amino or a protected amino group, R2 is amino or acylamino and R3 is carboxy or a protected carboxy group or a pharmaceutically acceptable salt thereof.
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