Lonza Ag

Lonza Inc.

Colm O'Murchu

Walter Brieden

Eva Maria Urban

Laurent Duc

Olwen M Birch

Yves Guggisberg

Frank Brux

Pierre Bossard

Kay-Sara Etter

Christine Bernegger

John Gordon

Kurt Burgdorf

Knut Burgdorf

A process for the preparation of a racemic or optically active compound of the formula

Process for the preparation of a racemic or optically active 4-(hydroxymethyl)-2-cyclopentene derivative

A novel process for the preparation of (1S, 4R)- or (1R, 4S)-4-(2-amino-6-chloro-9H-purin-9-yl)-2 -cyclopentene-1-methanol of the formula

Process for the preparation of an enantiomer of a (1R, 4S) or (1S, 4R)-1-amino-4-(hydroxymethyl)-2-cyclopentene derivative

A novel process for the preparation of (1S,4R)- or (1R,4S)-4-(2-amino-6-chloro-9H-purin-9-yl)-2-cyclo-pentene-1-methanol of the formulae ##STR1## is described. This entails in the first stage (.+-.)-2-aza-bicyclo[2.2.1]hept-5-en-3-one of the formula ##STR2## being acylated to give a (.+-.)-2-azabicyclo[2.2.1]hept-5-en-3-one derivative of the general formula ##STR3## in which R.sup.1 denotes C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, aryl or aryloxy, the latter being reduced in the second stage to give a cyclopentene derivative of the general formula ##STR4## in which R.sup.1 has the stated meaning, the latter then being converted in the third stage biotechnologically into the (1R,4S)- or (1S,4R)-1-amino-4-(hydroxymethyl)-2-cyclopentene of the formula ##STR5## the latter being converted in the fourth stage with N-(2-amino-4,6-dichloro-5-pyrimidinyl)formamide of the formula ##STR6## into the (1S,4R)- or (1R,4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopente ne-1-methanol of the formulae ##STR7## and the latter being cyclized in the fifth stage in a known manner to the final product of the formula I or II.

Process for the preparation of (1S,4R)-  or (1R,4S)-

A novel process for the preparation of (1S,4R)- or (1R,4S)-4-(2-amino-6-chloro-9H-purin-9-yl)-2-cyclopentene-1-methanol of the formulae ##STR1## is described. This entails in the first stage (.+-.)-2-azabicyclo[2.2.1]hept-5-en-3-one of the formula ##STR2## being acylated to give a (.+-.)-2-azabicyclo[2.2.1]hept-5-en-3-one derivative of the general formula ##STR3## in which R.sup.1 denotes C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, aryl or aryloxy, the latter being reduced in the second stage to give a cyclopentene derivative of the general formula ##STR4## in which R.sup.1 has the stated meaning, the latter then being converted in the third stage biotechnologically into the (1R,4S)- or (1S,4R)-1-amino-4-(hydroxymethyl)-2-cyclopentene of the formula ##STR5## the latter being converted in the fourth stage with N-(2-amino-4,6-dichloro-5-pyrimidinyl)formamide of the formula ##STR6## into the (1S,4R)- or (1R,4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopente ne-1-methanol of the formulae ##STR7## and the latter being cyclized in the fifth stage in a known manner to the final product of the formula I or II.

Enantiomer compositions of

A process, which is harmless with respect to safety, for the production of malonic acid anhydride. For this purpose, diketene is ozonized in the presence of a suitable carbonyl compound. Malonic acid anhydride is a highly reactive intermediate product for the synthesis of numerous active ingredients for, e.g., pharmaceutical agents, pesticides or dyes.

Process for the production of malonic acid anhydride

Process for the preparation of 2-substituted 5-nitroso-4,6-diaminopyrimidines. Malonic dinitrile and amidine are nitrosated in the presence of a nitrite salt, to form the corresponding amidine salt of isonitrosomalononitrile. The latter is converted to the end product in the presence of an aprotic polar solvent by heat treatment in a basic medium.

Process for the preparation of 2-substituted

This process involves the production of indole by catalytic dehydrocyclization. The process includes reacting, without the addition of free oxygen and/or a gas containing free oxygen, reacting o-ethylaniline and/or o-aminostyrene with steam in the presence of a particular catalyst. The catalyst contains at least one alkali compound and/or at least one alkaline earth compound and/or at least one compound containing iron, cobalt, chromium, vanadium, titanium, zinc, copper and/or zirconium.

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Colm O'Murchu