Lonza Ag

Lonzo Ltd.

Michael Petersen

Walter Brieden

Jean-Paul Roduit

Eva Maria Urban

Christine Bernegger-Egli

Katja Berchtold

Holger Breitbach

Josef Schr&ouml;er

Josef Schroer

Sakayu Shimizu

Klaus Heinzmann

Olwen M Birch

Kay-Sara Etter

Josef Schröer

Andreas Kjener

Marie-Luise Hischier

Susanne Thöni

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.

Process for the preparation of aminoalcohol derivatives and their further conversion to (1R, 4S)-4(2-amino-6-chloro-5-formamido-4- pyrimidinyl)-amino-2-cyclopentenyl-1-methanol

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.

Process for the preparation of aminoalcohol derivatives and their further conversion to (1R, 4S)-4(2-amino-6-chloro-5-formamido-4-pyrimidinyl)-amino-2-cyclopentenyl-1-methanol

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)&#x2014; 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.

Process for the preparation of aminoalcohol derivatives and their further conversion to (1R,4S)-4-(2-amino-6-chloro-5-formamido-4-pyrimidinyl)-amino)-2-cyclopentenyl-1-methanol

The invention relates to a biotechnological method for producing trifluoro-3(R)-hydroxybutyric acid derivatives of the general formula (I), where Rrepresents &#x2014;OR, where Ris hydrogen, Calkyl, Calkenyl, Ccy-cloalkyl, aryl, alkoxyalkyl or alkoxyalkoxyalkyl; &#x2014;NRR, where Rand Rare the same or different and represent hydrogen, Calkyl, Calkenyl, Ccycloalkyl or aryl; or &#x2014;SR, where Rrepresents hydrogen, Calkyl, Calkenyl, aryl or Ccycloalkyl, based on a trifluoroacetoacetic acid derivative of the general formula (II), where Rhas the meaning given above, by means of micro-organisms which are able to reduce a carbonyl function or by means of a cell-free enzyme extract of said micro-organisms.

Method for producing trifluoro-3(r)-hydroxybutyric acid derivatives

Process for the preparation of aminoalcohol derivatives and their further conversion to (1R,4S)-4-((2-amino-6-chloro-5-formamido-4-pyrimidinyl)-amino)-2-cyclopentenyl-1-methanol

The invention discloses a new method for producing enantiomer-enriched 1-amino-4-(hydroxymethyl)-cyclopent-2-ene derivatives of the general formulae (I) and (II) in which R is hydrogen or a possibly substituted C alkyl radical, aryl radical or cycloalkyl radical and R is acyl. According to said method a racemic 1-amino-4-(hydroxymethyl)-cyclopent-2-ene derivative of general formula (III), in which R has the meaning given above, is converted using a hydrolase and in the presence of an acylation agent

Process for preparing optically active 1-amino-4-(hydroxymethyl) cyclopent-2-ene derivatives

Process for the preparation of aminoalcohol derivatives and their further conversion to (1R, 4S)-4-((2-amino-6-chloro-5-formamido-4-pyrimidinyl)-amino)-2-cyclopentenyl-1-methanol

Biotechnological process for preparing N-acetylmannosamine

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Michael Petersen