- Preparation method of beta-homoglutamic acid
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The invention belongs to the field of preparation of organic compounds, and provides a preparation method of beta-homoglutamic acid. The method is characterized in that: 3-cyclohexenecarboxylic acid is used as a raw material, beta-homoglutamic acid is synthesized at a high yield through three the steps of reactions of Curtius rearrangement, olefin oxidation and protection group removal, and beta-homoglutamic acid with high yield and high optical purity can be obtained through configuration retention by using optically pure 3-cyclohexenecarboxylic acid. The method has the advantages of easily available raw materials, mild reaction conditions and low cost, and is suitable for large-scale preparation of beta-homoglutamic acid.
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Paragraph 0008; 0019; 0022
(2020/11/05)
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- METHOD FOR SYNTHESIS OF KETO ACID OR AMINO ACID BY HYDRATION OF ACETHYLENE COMPOUND
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An object of the present invention is to provide a method for synthesis of keto acids by hydration of an acetylene compound (acetylene-carboxylic acids) under mild conditions free from harmful mercury catalysts and a method for synthesis of amino acids from acetylene-carboxylic acids in a single container (one-pot or tandem synthesis). In one embodiment of the method according to the present invention for synthesis of keto acids, acetylene-carboxylic acids is hydrated in the presence of a metal salt represented by General Formula (1), where M1 represents an element in Group VIII, IX, or X of the periodic table, and X1, X2, or X3 ligand represents halogen, H2O, or a solvent molecule, and k represents a valence of a cation species, and Y represents an anion species, and L represents a valence of the anion species, and each of K and L independently represents 1 or 2, and k × m = L × n.
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Page/Page column 24
(2008/12/06)
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- Process for producing alpha 2,3/ alpha 2,8-sialyltransferase and sialic acid-containing complex sugar
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The present invention can provide a process for producing a protein having α2,3/α2,8-sialyltransferase activity using a transformant comprising a DNA encoding a protein having α2,3/α2,8-sialyltransferase activity derived from a microorganism belonging to the genus Pasteurella and a process for producing a sialic acid-containing complex carbohydrate using a transformant capable of producing a protein having α2,3/α2,8-sialyltransferase activity derived from a microorganism.
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- Human CDR-grafted antibody and antibody fragment thereof
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A human CDR-grafted antibody or the antibody fragment thereof which specifically reacts with the extracellular region of human CC chemokine receptor 4 (CCR4) but does not react with a human blood platelet; a human CDR-grafted antibody or the antibody fragment thereof which specifically reacts with the extracellular region of CCR4 and has a cytotoxic activity against a CCR4-expressing cell; and a medicament, a therapeutic agent or a diagnostic agent comprising at least one of the antibodies and the antibody fragments thereof as an active ingredient.
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- Gene recombinant antibody and antibody fragment thereof
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A recombinant antibody or the antibody fragment thereof which specifically reacts with an extracellular domain of human CCR4; a DNA which encodes the recombinant antibody or the antibody fragment thereof; a method for producing the recombinant antibody or the antibody fragment thereof; a method for immunologically detecting CCR4, a method for immunologically detecting a cell which expressed CCR4 on the cell surface, a method for depleting a cell which expresses CCR4 on the cell surface, and a method for inhibiting production of Th2 cytokine, which comprise using the recombinant antibody according or antibody fragment thereof; a therapeutic or diagnostic agent for Th2-mediated immune diseases; and a therapeutic or diagnostic agent for a blood cancer.
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- Azapeptides useful in the treatment of Hepatitis C
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The present invention relates to azapeptide compounds represented by the formula: pharmaceutical compositions containing such compounds, and the use thereof in the treatment of Hepatitis C viral infections.
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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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- Peptides with an insulin-like action
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Peptides with an insulin-like action, of formula I: STR1 in which G is a hydrogen atom, an amino add residue, or a monosubstituted or polysubstituted amino acid; D is an amino acid residue, a phosphoamino acid residue, a monosaccharide residue, or a covalent bond; E is --NH--(CH2)n --NR52, a glycerol residue, or --NH--(CH2)p --R6 --R7 ; R1 is (C1 -C4)-alkyl or =O; R2 is a sulfhydryl protecting group, (C1 -C3)-alkyl, or a hydrogen atom; R3 and R4, independently of one another, are a hydrogen atom or methyl; R5, each being identical or different, is a hydrogen atom, 1 to 6 monosaccharide residues, or 1 to 6 monosubstituted or polysubstituted monosaccharide residues; R6 is O PO4 H, PO2 H, NHCOO, S or OCOO; R7 is a hydrogen atom, 1 to 6 monosaccharide residues, or 1 to 6 monosubstituted or polysubstituted monosaccharide residues; w is an integer 1 or 2; their preparation and use for treatment of diabetes mellitus or insulin-independent diabetes.
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- Primordial Amino Acids by Reductive Amination of α-Oxo Acids in Conjunction with the Oxidative Formation of Pyrite
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The theory of an autotrophic origin of life postulates a primordial formation of amino acids by a mild and specific chemical energy source, namely by the reductive amination of α-oxo acids in conjunction with the oxidative formation of pyrite.Here we show experimental proof for this reaction, which involves carbon dioxide as catalyst.
- Hafenbradi, D.,Keller, M.,Waechtershaeuser, G.,Stetter, K. O.
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p. 5179 - 5182
(2007/10/02)
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- Asymmetric Catalysis by Vitamin B12: The Isomerization of Achiral Aziridines to Optically Active Allylic Amines
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Achiral N-acylaziridines are isomerized to optically active N-acyl-allylamines in ee's of up to 95percent by catalytic amounts of cob(I)alamin in MeOH.
- Zhang, Zhong da,Scheffold, Rolf
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p. 2602 - 2615
(2007/10/02)
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- Remarkable Nucleophilic Activity of N-Acetamido Group. Synthesis of Proline and Lysine for Biosynthetic Purposes
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DL-Proline 7 was prepared from acroleine 1 and diethyl N-acetylaminomalonate 2 in 22percent overall yield.The key step was an intramolecular substitution of tosyloxy group in 4b by N-acetylamino group.The tosylate 4b was also an intermediate in synthesis of (6-13C) lysine.Pronounced differences in incorporation of (6-13C) and lysine to lupanine 12 were observed.
- Golebiewski, W. Marek
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p. 425 - 430
(2007/10/02)
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- Chemical Conversion of Cyclic α-Amino Acids to α-Aminodicarboxylic Acids by Improved Ruthenium Tetroxide Oxidation
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The ruthenium tetroxide (RuO4) oxidation of N-acylated L-proline esters, prepared from L-proline, was carried out under two-phase conditions to afford good yields of the corresponding lactams with no appreciable racemization, and the products were hydrolyzed in aqueous hydrochloric acid to L-glutamic acid.Similar transformation starting with racemic 2-piperidinecaboxylic acid and 2-azetidinecarboxylic acid gave 2-aminoadipic acid and aspartic acid, respectively.A novel chemical converion of cyclic α-amino acids into α-aminodicarboxylic acids has been accomplished.A new solvent system, ethyl acetate-water, was developed for this two-phase oxidation.It was found to be very useful in reducing the necessary reaction time.Keywords --- oxidation; regioselectivity; lactam synthesis; ruthenium tetroxide; cyclic α-amino acid; α-aminodicarboxylic acid; L-proline; L-glutamic acid; two-phase method; ethyl acetate-water system
- Yoshifuji, Shigeyuki,Tanaka, Ken-ichi,Kawai, Tomoyuki,Nitta, Yoshihiro
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p. 5515 - 5521
(2007/10/02)
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- FLAME-INDUCED CARBOXYLATION OF UNSATURATED AMINES IN AN AQUEOUS FORMIC ACID SOLUTION
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When a hydrogen-oxygen flame was kept in contact with an aqueous formic acid solution of unsaturated amines, carboxylation onto a double bond took place.This reaction revealed to be initiated by addition of a hydrogen atom to the double bond followed by coupling of the resulted substrate radical with a carboxyl radical.
- Nomoto, Shinya,Harada, Kaoru
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p. 145 - 148
(2007/10/02)
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- Medical process and preparation
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A medication and method of treatment for reducing tissue trauma in an animal, comprising the use of a N,N-dimethyl aspartic acid and/or N,N-dimethyl glutamic acid, physiologically acceptable salt or salts of either of the foregoing, and/or a mixture or mixtures of the foregoing, in which a suitable maskant such as benzyl alcohol may be included, the preferable method of treatment being a topical application to the skin to achieve penetration into the areas of tissue trauma.
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- Synthesis of α-Aminoadipic Acid
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A two-step synthesis of α-aminoadipic acid in quite encouraging yield through reduction and hydrolysis of azlactone of succinic anhydride with hydriodic acid in presence of red phosphorus has been reported.
- Khan, Naseem H.,Ali, Mohd.,Panda, H.,Rakhshinda,
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p. 1077 - 1078
(2007/10/02)
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