- Method for synthesizing meglumine through catalytic hydrogenation by taking ammonia borane as hydrogen source
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The invention discloses a method for synthesizing meglumine through catalytic hydrogenation by taking ammonia borane as a hydrogen source, and belongs to the technical field of chemical drug synthesis. The method comprises the step that on the basis that glucose-methylamine schiff base is synthesized by taking glucose and methylamine as raw materials, and by taking ammonia borane as the hydrogen source for performing catalytic hydrogenation, the meglumine is synthesized. Compared with a method in the past, the method has the advantages of being mild in catalytic hydrogenation reaction, safe and high yield.
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Paragraph 0020-0022; 0025
(2018/10/19)
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- Low-Temperature Reductive Aminolysis of Carbohydrates to Diamines and Aminoalcohols by Heterogeneous Catalysis
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Short amines, such as ethanolamines and ethylenediamines, are important compounds in today's bulk and fine chemicals industry. Unfortunately, current industrial manufacture of these chemicals relies on fossil resources and requires rigorous safety measures when handling explosive or toxic intermediates. Inspired by the elegant working mechanism of aldolase enzymes, a novel heterogeneously catalyzed process—reductive aminolysis—was developed for the efficient production of short amines from carbohydrates at low temperature. High-value bio-based amines containing a bio-derived C2 carbon backbone were synthesized in one step with yields up to 87 C%, in the absence of a solvent and at a temperature below 405 K. A wide variety of available primary and secondary alkyl- and alkanolamines can be reacted with the carbohydrate to form the corresponding C2-diamine. The presented reductive aminolysis is therefore a promising strategy for sustainable synthesis of short, acyclic, bio-based amines.
- Pelckmans, Michiel,Vermandel, Walter,Van Waes, Frederik,Moonen, Kristof,Sels, Bert F.
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p. 14540 - 14544
(2017/10/23)
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- Mixed Sugar Compositions
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Novel mixtures of sugar amides or sugar amines are disclosed that have improved thermal properties over the individual components. New feedstocks based on both the surfactant tail as well as the sugar head group allow for improved physical properties of sugar amide surfactant mixtures and thus improved formulatability. Furthermore, new sources of unique methyl esters from both bioengineering and or co-metathesis of fats and oils provide novel and improved sugar amide surfactant mixtures.
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Paragraph 0207
(2014/09/29)
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- An efficient renewable-derived surfactant for aqueous esterification reactions
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An efficient and simple approach for the aqueous esterification of a range of carboxylic acids with alcohols has been developed using catalytic amounts of a glucose-derived N-alkanoyl-N-methyl-1-glycamine non-ionic biosurfactant (C12MG). Excellent yields to final products were obtained under mild conditions and the protocol was amenable to both aromatic and long alkyl chain acids (e.g. fatty acids).
- Rajabi, Fatemeh,Luque, Rafael
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p. 5152 - 5155
(2014/01/23)
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- Composition and Tablet Comprising Raltegravir
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The present invention relates to a composition and tablet comprising raltegravir and to a process for the preparation of such tablet.
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- Water-soluble porphyrin derivatives for photodynamic therapy, their use and manufacture
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High purity pharmaceutical-grade water-soluble porphyrin derivatives given by formula 1 or 2 in the specification, and new methods to prepare and use such porphyrin derivatives are disclosed. A preferred method comprises the steps of one- or two-step direct acidic alcoholysis of biological raw material producing a crystalline alkyl pheophorbide, conversion of the obtained alkyl pheophorbide into an acidic porphyrin, and reaction of the acidic porphyrin in water or in an aqueous organic solution with a hydrophilic organic amine. Another preferred method comprises reaction of acidic porphyrins prepared in water or in aqueous organic solution with a hydrophilic organic amine. Another preferred method comprises the additional step of purification of the resultant water-soluble porphyrin derivative by reversed phase chromatography using volatile solvents. The disclosed compounds are useful as photosensitizers for the photodynamic therapy of cancer, infectious and other diseases as well as for light irradiation treatments in other cases.
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- Water-soluble porphyrin derivatives for photodynamic therapy, their use and manufacture
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High purity pharmaceutical-grade water-soluble porphyrin derivatives having a general formula given by formula 1 or 2 and new methods to prepare and use such porphyrin derivatives: Wherein B is a ring having the structure: Wherein: R1═—CH═CH2, —CH(OAlk)CH3, —CHO, —C(O)CH3, —CH2CH3, —CH(Alk)CH(COAlk)2, —CH2CH(COAlk)2, —CH(Alk)CH2COAlk, —CH(Alk)CH2CH(OH)CH3, and —CH2CH2CH(OH)CH3 R2═—CH3, —CHO, —CH(OH)Alk, —CH═CHAlk, CH2OH, and CH2OAlk; R3═—OH, —OAlk, —NH-Alk, NH—X—COO?(HG)+, —NH—Y—NR8R9, -and NH—Y—OH; R4═—OAlk, —NH-Alk, and NH—X—COO?(HG)+; R5═—OAlk, —NH-Alk, and NH—X—COO?(HG)+; R6═H and —COOAlk; R7═—O?(HG)+, —OAlk, —NH-Alk, and —NH—X—COO?(HG)+; R8═H and Alk R9═H and Alk Wherein: —NH—X—COO?=the residue of organic amino acid; X=alkylidene, peptides, oligopeptides and —(CH2CH2O)nCH2CH2—, wherein n=1-30; Y=alkylidene and —(CH2CH2O)nCH2CH2—, wherein n=1-30; G=a hydrophilic organic amine (fex. N-methyl-D-glucamine and other amino-group containing carbohydrate derivatives, TRIS, amino acids, oligopeptides); and Alk=an alkyl substituent. An embodiment of the present invention consists of a method to prepare water-soluble porphyrin derivatives comprising the steps of one- or two-step direct acidic alcoholysis of biological raw material producing a crystalline alkyl pheophorbide, conversion of the obtained alkyl pheophorbide into an acidic porphyrin, and reaction of the acidic porphyrin in water or in an aqueous organic solution with a hydrophilic organic amine. Another embodiment of the present invention consists of a method to prepare water-soluble porphyrin derivatives, comprising reaction of acidic porphyrins prepared by any known method in water or in aqueous organic solution with a hydrophilic organic amine. Another embodiment of the present invention comprises the additional step of purification of the resultant water-soluble porphyrin derivative by reversed phase chromatography using volatile solvents. The compound disclosed in the present invention can be used as photosensitizers for the photodynamic therapy of cancer, infectious and other diseases as well as for light irradiation treatments in other cases.
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- Beta-lactams having an alkyl-substituted side chain
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Taxane derivatives having an alkyl substituted C13 side chain.
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- Process for the preparation of N-alkypolyhydroxyalkylamines from monoalkylamine and reducing sugar
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Aqueous, alcoholic or aqueous-alcoholic solutions of a monoalkylamine and a reducing sugar are simultaneously injected into a mixing unit and the two solutions are mixed under turbulence in the mixing unit for 6 seconds to 5 minutes at a temperature of 25 to 60° C. and a pressure of 50 to 90 bar. The mixture is then added to a hydrogenation reactor and hydrogenated with hydrogen in the presence of a hydrogenation catalyst. An alkylpolyhydroxyalkylamine is obtained in high yield and with high purity.
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Page column 4-5
(2008/06/13)
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- Chelated complexes of paramagnetic metals with low toxicity
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Compounds of formulae (I) and (II) wherein the R, R1, R2, R3 and R4 groups have the meanings defined in the disclosure, are useful chelants for metal ions. The complexes of compounds (I) and (II) with paramagnetic ions are useful as contrast agents for M.R.I. imaging.
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- Tricyclic taxanes having an alkoxy, alkenoxy or aryloxy substituted side-chain and pharmaceutical compositions containing them
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Taxane derivatives having an alkoxy, alkenoxy or aryloxy substituted C13 side chain.
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- C2 tricyclic taxanes
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Taxane derivatives having alternative C2 substituents.
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- Tricyclic taxanes having a butenyl substituted side-chain and pharmaceutical compositions containing them
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Taxane derivatives having a 3' butenyl substituted C13 side chain.
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- C10 tricyclic taxanes
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Taxane derivatives having alternative C10 substituents.
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- Scavenger assisted combinatorial process for preparing libraries of amides, carbamates and sulfonamides
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This invention relates to a novel solution phase process for the preparation of amide, carbamate, and sulfonamide combinatorial libraries. These libraries have utility for drug discovery and are used to form wellplate components of novel assay kits.
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- Chelated complexes of paramagnetic metals with low toxicity
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Compounds of formulae (I) and (II) wherein the R, R1, R2, R3and R4groups have the meanings defined in the disclosure, are useful chelants for metal ions. The complexes of compounds (I) and (II) with paramagnetic ions are useful as contrast agents for M.R.I. imaging.
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- Taxanes having a pyridyl substituted side-chain and pharmaceutical compositions containing them
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Taxane derivatives having a 3' pyridyl substituted C13 side chain.
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- Carbohydrate-derived surfactants and their precursors
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A method for the manufacture of N,N dialkylglycamine compounds of general formula R2 NR1 R3 (I) by reacting a secondary amine of general formula R2 NHR3 (II) in which R2 is a straight or branched chain alkyl or hydroxyalkyl group having from 1 to 4 carbon atoms and R3 is a residue from a monosaccharide, with an alkali metal or alkaline earth metal aliphatic sulphate, R1 SO4 M, in which R1 is a straight or branched chain alkyl or alkenyl group having from 8 to 24 carbon atoms. The betaine, suphobetaine and N-oxidised derivatives of (I) are provided for use as mild surfactants.
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- Preparation of substituted isoserine esters using β-lactams and metal or ammonium alkoxides
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A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal or an ammonium alkoxide is reacted with a β-lactam.
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- Furyl or thienyl carbonyl substituted taxanes and pharmaceutical compositions containing them
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Taxane derivatives of the formula STR1 wherein R1 is phenyl or p-nitrophenyl, R3 is furyl or thienyl, T1 is hydrogen, hydroxyl protecting group, or --COT2, T2 is H, C1 -C6 alkyl, C2 -C6 alkenyl, C2 -C6 alkynyl or monocylic aryl, Ac is acetyl, and E1 and E2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.
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- Butenyl substituted taxanes and pharmaceutical compositions containing them
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Taxane derivatives of the formula STR1 wherein R1 is butenyl, R3 is phenyl, T1 is hydrogen, hydroxyl protecting group, or --COT2, T2 is H, C1 -C6 alkyl, C2 -C6 alkenyl, C2 -C6 alkynyl or monocylic aryl, Ac is acetyl, and E1 and E2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.
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- Cyclohexyl substituted taxanes and pharmaceutical compositions containing them
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Taxane derivatives of the formula STR1 wherein R1 is cyclohexyl, R3 is phenyl, T1 is hydrogen, hydroxyl protecting group, or --COT2, T2 is H, C1 -C6 alkyl, C2 -C6 alkenyl, C2 -C6 alkynyl or monocylic aryl, Ac is acetyl, and E1 and E2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.
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- Furyl and thienyl substituted taxanes and pharmaceutical compositions containing them
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A taxane derivative of the formula STR1 wherein STR2 Z is --OT 1, T 1 is hydrogen, hydroxyl protecting group, or --COT 2,T 2 is H, C 1 -C 6 alkyl, C 1 -C 6 alkenyl, C 1 -C 6 alkynyl or monocylic aryl,R 3 is benzoyl, substituted benzoyl or C 1 -C 6 alkoxycarbonyl,Ac is acetyl, andE 1 and E 2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.
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- Certain alkoxy substituted taxanes and pharmaceutical compositions containing them
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A taxane derivative of the formula STR1 wherein R1 is phenyl or substituted phenyl, R3 is CH3 O--, or CH3 CH2 O--, Z is --OT1, T1 is hydrogen, hydroxyl protecting group, or --COT2. T2 is H, C1 -C6 alkyl, C1 -C6 alkenyl, C1 -C6 alkynyl or monocylic aryl, Ac is acetyl, and E1 and E2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.
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- Certain substituted taxanes and pharmaceutical compositions containing them
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A taxane derivative of the formula STR1 wherein R1 and R3 are independently selected from the group comprising phenyl, naphthalene, C6 H5 CHCH--, and STR2 provided, however, R1 and R3 are not both phenyl; Q is CH3 --, (CH3)3 C--, CH3 O--, Cl, Br, F, NO2, STR3 Z is --OT1, T1 is hydrogen, hydroxyl protecting group, or --COT2, T2 is H, C1 -C6 alkyl, C1 -C6 alkenyl, C1 -C6 alkynyl or monocylic aryl, Ac is acetyl, and E1 and E2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.
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- Water soluble, antineoplastic derivatives of taxol
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Antineoplastic, water soluble, taxol derivatives and methods for preparing the same are described.
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- Novel nitrosourea compounds and process for preparing the same
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A nitrosourea compound of the formula: STR1 wherein R1 is alkyl of one to six carbon atoms, hydroxyalkyl of one to six carbon atoms, alkenyl of three to five carbon atoms or alkynyl of three to five carbon atoms, R2 is aldopentofuranosyl, aldo-pentopyranosyl, aldo-hexopyranosyl, O-aldo-hexopyranosyl-(1→4)-aldo-hexopyranosyl or a group of the formula: --CH2 (CHOH)n CH2 OH, and wherein n is zero or an integer of one to four. A method of preparation is disclosed whereby said nitrosourea compound is prepared by the nitrosation of a compound of the formula: STR2 wherein R1 and R2 are the same as above. Said nitrosourea compound is useful as an anti-tumor or anti-leukemic agent.
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- Skin treating cosmetic compositions containing N-polyhydroxyalkyl-amines
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The present invention relates to compositions for the treatment of the skin containing up to 25% by weight of at least one N-polyhydroxyalkyl-amine of the formula STR1 wherein R1 is hydrogen, lower alkyl, hydroxy-lower alkyl or aminoalkyl, as well as heterocyclic aminoalkyl, R is the same as R1 except that both cannot be hydrogen at the same time, R2 is --CH2 OH or --COOH, m is the integer 3 or 4, and n is the integer O, or, when m is 3 and R2 is --CH2 OH, 1; and the method of skin treatment therewith.
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- Process for converting esters to amine salts
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A new method for converting certain diesters to physiologically acceptable amines which comprises reacting the diester with the desired amine in a solvent consisting essentially of water.
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