122-87-2Relevant academic research and scientific papers
Process for preparing 5-arylhydantoins using 5-hydantoin, a halogenating agent and p-phenol
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, (2008/06/13)
The present invention provides a novel process for the preparation of 5-arylhydantoins as an important intermediate of (D)-arylglycines (e.g., (D)-p-hydroxyphenyl-glycine) useful for the synthesis of semisynthetic penicillines and cephalosporins, the process comprising (i) reacting a 5-unsubstituted hydantoin compound with a halogenating agent and (ii) reacting the resulting product with a p-unsubstituted phenol compound, the hydroxy group of which may be protected, to substitute the 5-position of the hydantoin compound with the phenol compound at the para position.
Process for preparing an α-amino acid, the corresponding ester and amide
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, (2008/06/13)
Process for preparing an a-amino acid having the general formula (1) of STR1 where R represents an aryl group or a substituted aryl, cycloalkyl or alkyl group, in which process glyoxylic acid, or a precursor or derivative thereof, is contacted in the presence of sulphamic acid with an unsaturated compound chosen from the group of aromatics, cycloalkenes and alkenes. By applying the process higher efficiencies are obtained. The acid obtained as reaction product can be esterified and amidated without prior isolation.
Polyunsaturated fatty acid derivatives, pharmaceutical compositions containing the same, method for the preparation thereof, and their use as medicament
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, (2008/06/13)
The compounds of the Formula (I) STR1 wherein R1 is a C18-24 alkenyl containing at least two double bonds, or --(CH2)n --CH(NH2)m --COOH X is 0, NH or C1-4 alkyl-N, Y is CONH2, COOH or COOMe, wherein Me is hydrogen metal, and R2 is a side chain of a any amino acid except L-GLU or L-ASP at α-position or a group of Formula wherein k is zero or an integer of 1, n is zero or an integer of 1 to 3, m is zero or an integer of 1 to 4, A is hydroxyl or one A is hydroxyl and the other A is hydrogen. M is H or R1 --CO and X and R1 are as defined above and their salts having tyrosine kinase inhibitor activity can be used as antitumor agents.
Formation of hydroxyaromatic ketoacetal from a hydroxyaromatic methylketone and production of 5-(4'-hydroxyphenyl)hydantoin and Dp-hydroxyphenylglycine from 4-hydroxyacetophenone
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, (2008/06/13)
The present invention provides a method for producing a hydroxyaromatic ketoacetal from a hydroxyaromatic methylketone. The invention further provides a method for producing a hydroxyaromatic ketoaldehyde from a hydroxyaromatic ketoacetal. The hydroxyaromatic ketoaldehyde can be further reacted to form a hydantoin, which hydantoin can be hydrolyzed to produce a hydroxyphenylglycine.
Novel spergualin-related compounds and compositions
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, (2008/06/13)
The present invention relates to novel spergualin-related compounds represented by the general formula [I]: STR1 wherein X is --(CH2)1?5 or STR2 Y is a hydrogen atom or a residue obtained by removing a hydroxyl group from the carboxyl group of an amino acid or a peptide; m is 0, 1 or 2 and n is 1 or 2, with the proviso that Y is not a hydrogen atom when n is 2 and m is 0. This compounds are stable and exhibit a high immunosuppressive activity.
Stereoselective resolution of phenylglycine derivatives with enzyme resins
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, (2008/06/13)
The invention relates to a process for the stereo-selective resolution of DL-phenylglycine derivatives by hydrolyzing the ester or amide groups of N-acyl-L-phenylglycine esters or amides in N-acyl-DL-phenylglycine esters or amides by the action of enzymes, separating the N-acyl-D-phenylglycine esters or amides from the N-acyl-L-phenylglycines and then, if appropriate, subjecting the ester or amide groups of the D-enantiomers and the acyl groups to acid hydrolysis, characterized in that enzyme which are bonded to carriers are allowed to act on the N-acyl-DL-phenylglycine esters or amides in an inert two-phase mixture consisting of water-immiscible organic solvent and water.
Cephalosporins
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, (2008/06/13)
Cephalosporins of the formula STR1 wherein A is phenyl, 4-hydroxyphenyl, cyclohexyl, cyclohexene-1-yl, cyclohexa-1,4-diene-1-yl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl or 3,4-disubstituted phenyl, where the substituents, which may be identical to or different from each other, are each chlorine, hydroxyl or methoxy; Y is hydrogen or methoxy; D is hydrogen, hydroxyl, acetoxy, aminocarbonyloxy, pyridinium, aminocarbonyl-pyridinium or the group S-Het, where Het is 1-methyl-tetrazol-5-yl, tetrazol-5-yl, 3-methyl-1,2,4-thiadiazol-5-yl, 1,2,4-thiadiazol-5-yl, 1,3,4-thiadiazol-5-yl, 2-methyl-1,3,4-thiadiazol-5-yl, 2-methylamino-1,3,4-thiadiazol-5-yl, 2-dimethylamino-1,3,4-thiadiazol-5-yl, 2-formylamino-1,3,4-thiadiazol-5-yl, 2-acetylamino-1,3,4-thiadiazol-5-yl, 2-methyl-1,3,4-oxadiazol-5-yl, 1,2,3-triazol-4-yl or 1,2,4-triazol-3-yl; R is hydrogen, methyl, cyclopropyl, hydroxyl, methoxy, ethoxy, mercapto, morpholino, thiomorpholino, thiomorpholino-S-oxide, thiomorpholino-S,S-dioxide, STR2 E is hydrogen or a protective group which is easily removable in vitro or in vivo; and nontoxic, pharmacologically acceptable salts thereof.
Process for preparing p-hydroxy phenylglycine
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, (2008/06/13)
The disclosure relates to a process for converting p-hydroxymandelic acid or a salt thereof to p-hydroxyphenylglycine. The product is a useful intermediate in the pharmaceutical industry.
4-Tert.-butoxyphenylglycinonitrile and the preparation of D-(-)- and L-(+)-4-hydroxyphenylglycine
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, (2008/06/13)
4-Tert.-butoxyphenylglycinonitrile (I) STR1 and a process for the preparation of D-(-)-4-hydroxyphenylglycine (IIa) and L-(+)-4-hydroxyphenylglycine (IIb) STR2 wherein compound I is reacted in a conventional manner, in alcoholic solution and in the presence of a carbonyl compound, with about the equimolar amount of L-(+)-tartaric acid or D-(-)-tartaric acid and the D-(-)-I-L-(+)-tartrate or L-(+)-I-D-(-)-tartrate thereby obtained in crystalline form is converted to IIa or IIb respectively in aqueous acid solution at 20°-110° C. by splitting off the L-(+)-tartaric acid or D-(-)-tartaric acid, hydrolyzing the nitrile group and hydrolytically splitting off the tert.-butyl group.
Process for resolution of racemic DL-α-aminocarboxylic acids
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, (2008/06/13)
In a process for resolving racemic DL-α-aminocarboxylic acids the said acids are reacted in an inert solvent with an aromatic o-hydroxy aldehyde to obtain an azomethine derivative which is reacted in the same stage with an optically active amine base to give a salt. The diastereomeric salt obtained is separated and the respective optically active α-aminocarboxylic acid is obtained therefrom by an acid treatment. By this process aliphatic and aromatic α-amino-carboxylic acids can be resolved, especially p-hydroxyphenyl glycine.
