Abstract: A novel method for synthesizing a Hirulog peptide is devised.

Abstract: A method for the production of acetals and ketals of 3-amino-5-(hydroxymethyl) cyclopenlane-1,2-diols of formula (I): (and/or the enantiomer), where R1 is H, C1-6-alkyl, C3-8-cycloalkyl or benzyl and (i) R2 is methyl and R3 is ethyl, (ii) R2 is H and R3 is C1-6-alkyl or phenyl or (iii) R2 and R3 together form a group of formula —(CH2)n— with n=4 to 6, present as free amines or as salts of di- or tri-basic organic acids, starting from 2-acetyl-2-aza-bicyclo[2.2.1]hept-5-en-3-one of formula (II): (and/or the enantiomer). The method is equally useful, depending on the starting material, for the production of enantiomerically-pure compounds, or mixtures with arbitrary enantiomeric content.

Abstract: Method of peptide synthesis, comprising the steps of a. synthesizing a peptide linked to a solid phase which peptide comprises at least one cysteine, homo- or nor-cysteine residue, which cysteine is protected in its side chain by a S-tert.butyl-sulphenyl group b. either coupling N-terminally a further amino acid having a 3,3?-dithio-(1-carboxy-propyl)-propionyl-radical on its N? or deprotecting the N? of the N-terminal amino acid and reacting the free N? with 3,3?-dithio-propionic acid imide to yield the corresponding N?-3,3?-dithio-(1-carboxy-propyl)-propionamide or deprotecting the N? of the N-terminal amino acid and reacting the free N? with a compound of formula IV R7-S—S—[CH2]2—COOH IV wherein R7 is aryl-, including heteronuclear aryl, or is aralkyl-, alkylaryl- or alkyl-, which may be further substituted with halogeno, amido, ester, carboxy or ether, and c. reacting the peptide with a S-tert.Butyl-sulphenyl-protection group removing reagent, and d.

Abstract: A novel for amidation of C-terminal carboxyl groups of peptides is devised, which methods avoids undesired epimerisation of the ?-carbon of the C-terminal amino acid yielding diastereoisomeric variants of the amidated peptide.

Abstract: The invention relates to a novel process for the preparation of (1R,4S)- or (1S,4R)-1-amino-4-(hydroxy-methyl)-2-cyclopentene of the formulae and/or of (1S,4R)- or (1R,4S)-amino alcohol derivatives of the general formulae and to novel microorganisms which are able to utilize a cyclopentene derivative of the general formula as sole nitrogen source, as sole carbon source or as sole carbon and nitrogen source.

Abstract: A novel method for on-resin formation of disulfide-borne cyclization of peptides is devised.

Abstract: The invention relates to a novel process for the preparation of an aminoalcohol of the formula racemically or optically active, starting from 2-azabicyclo[2.2.1]hept-5-en-3-one, its further conversion to give the corresponding acyl derivative and its further conversion to (1S,4R)- or (1R,4S)-4-(2-amino-6-chloro-9-H-purine-9-yl)-2-cyclopentenyl-1-methanol of the formulae In the latter synthesis, the aminoalcohol is converted into the corresponding D- or L-tartrate, which is then reacted with N-(2-amino-4,6-dichloropyrimidin-5-yl) formamide of the formula to give (1S,4R)- or (1R,4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentenyl-1-methanol of the formulae and then cyclized to give the end compounds.

Abstract: A method for the production of 6,6,6-trihalo-3,5-dioxohexanoic acid esters of formula (I): in addition to the enols thereof and <I>E</I> and <I>Z</I> isomers, wherein X independently represents fluorine, chlorine or bromine and R1 represents alkyl, cycloalkyl, aryl or aralkyl. A method for the production of enol ethers of formula (Ib): and the enols thereof (E and Z isomers) wherein X and R1 have the above-mentioned meanings.

Abstract: The invention relates to a novel process for the preparation of an aminoalcohol of the formula racemically or optically active, starting from 2-azabicyclo[2.2.1]hept-5-en-3-one, its further conversion to give the corresponding acyl derivative and its further conversion to (1S,4R)- or (1R,4S)-4-(2-amino-6-chloro-9-H-purine-9-yl)-2-cyclopentenyl-1-methanol of the formulae In the latter synthesis, the aminoalcohol is converted into the corresponding D- or L-tartrate, which is then reacted with N-(2-amino-4,6-dichloropyrimidin-5-yl)formamide of the formula to give (1S,4R)- or (1R,4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentenyl-1-methanol of the formulae and then cyclized to give the end compounds.

Abstract: N-Aryl or N-heteroarylformamides are prepared by hydrogenating a corresponding nitroarene or nitroheteroarene with formic acid and/or ammonium formate as hydrogen donor and formylating agent in the presence of at least one noble metal-based hydrogenation catalyst and a vanadium or molybdenum compound as co-catalyst.

Abstract: The present invention provides for microorganisms capable of tolerating acetonitrile concentrations of at least 3 M, enzyme extracts obtainable from these microorganisms, a nitrile hydratase obtainable from these microorganisms, a method for preparing amides using these microorganisms, the enzyme extracts or the nitrile hydratase obtainable therefrom, and a method for removing acetonitrile from solutions using these microorganisms, the enzyme extracts or the nitrile hydratase obtainable therefrom.

Abstract: A method for preparing, from at least one hygroscopic substance, mixtures that can be granulated and that have little hygroscopicity. The corresponding mixtures, especially carnitine-magnesium citrate and carnitine-magnesium hydroxycitrate, are produced.

Abstract: The invention relates to a novel process for the preparation of an aminoalcohol of the formula racemically or optically active, starting from 2-azabi-cyclo[2.2.1]hept-5-en-3-one, its further conversion to give the corresponding acyl derivative and its further conversion to (1S,4R)— or (1R,4S)-4-(2-amino-6-chloro-9-H-purine-9-yl)-2-cyclopentenyl-1-methanol of the formulae In the latter synthesis, the aminoalcohol is converted into the corresponding D- or L-tartrate, which is then reacted with N-(2-amino-4,6-dichloropyrimidin-5-yl) formamide of the formula to give (1S, 4R)- or (1R, 4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentenyl-1-methanol of the formulae and then cyclized to give the end compounds.

Abstract: A method for the production of acetals and ketals of 3-amino-5-(hydroxymethyl)cyclopentane-1,2-diols of formula (I): (and/or the enantiomer), where R1 is H, C1-6-alkyl, C3-8-cycloalkyl or benzyl and (i) R2 is methyl and R3 is ethyl, (ii) R2 is H and R3 is C1-6-alkyl or phenyl or (iii) R2 and R3 together form a group of formula —(CH2)n— with n=4 to 6, present as free amines or as salts of di- or tri-basic organic acids, starting from 2-acetyl-2-azabicyclo[2.2.1]hept-5-en-3-one of formula (II): (and/or the enantiomer). The method is equally useful, depending on the starting material, for the production of enantiomerically-pure compounds, or mixtures with arbitrary enantiomeric content.

Abstract: Cyanoacetamides of the formula: and corresponding salts thereof; N?-(cyanoacetyl)-L-histidines, of the formula: and salts, tautomers and esters thereof; and N?-(cyanoacetyl)-3-methyl-L-histidines of the formula: and salts and esters thereof.

Abstract: A starting product for the preparation of COX-2 inhibitors, notably the compound 1-(6-methylpyridine-3-yl)-2-[(4-(methylsulfonyl)phenyl]ethanone of the formula (I): A method for making the compound.

Abstract: A novel biotechnological process for the preparation of nitriles, starting from amides, is described. Micro-organisms of the genus Amycolatopsis, Actinomadura or Rhodococcus are employed for this process.

Abstract: The present invention relates to a novel process for the preparation of (S)— or (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid and to novel microorganisms capable of utilizing the propionamide of the formula in the form of the racemate or of its optically active isomers as the sole nitrogen source.

Abstract: The present invention relates to a novel process for the preparation of (S)- or (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid and to novel microorganisms capable of utilizing the propionamide of the formula in the form of the racemate or of its optically active isomers as the sole nitrogen source.

Abstract: A process for the production of acetylopyridines of the formula (1): by reacting a pyridinecarboxylic ester of the formula (II): wherein R1 is C1-6-alkyl, with acetic acid in the gas phase in the presence of a catalyst. The active material of the catalyst is titanium dioxide and at least one alkali or alkaline earth metal oxide, and it is supported on an alumina-silica support having an apparent porosity of at least 50 percent. The process has the advantage of producing only small amounts of by-products (e.g, pyidine).