Hoffmann-la Roche Inc.

Martin Karpf

Ren&eacute; Trussardi

Ulrich Zutter

Beat Wirz

Emil A Broger

Ivan Kompis

Rene Trussardi

René Trussardi

Stefan Abrecht

Markus Schlageter

Alfredo Guerrato

Hanny K Berger

The present invention relates to a process for the preparation of a 4,5-diamino shikimic acid derivative of formula and pharmaceutically acceptable addition salts thereofwherein

Process for the preparation of 4,5-diamino shikimic acid derivatives

The invention provides a multistep process for preparing 1,2-diamino compounds and pharmaceutically acceptable addition salts thereof from 1,2-epoxides.

Process for preparing 1,2-diamino compounds

The present invention is concerned with mixed anhydrides. The mixed anhydrides are prepared by adding an adjuvant base to a mixture of acid and reactive acid derivative. The mixed anhydrides play an role primarily in activating and coupling reactions.

Process for the preparation of mixed anhydrides

The present invention is concerned with an improved process for the manufacture of mixed anhydrides. The process comprises adding an adjuvant base to a mixture of acid and reactive acid derivative. It is especially suitable for use in the synthesis of peptides and/or for the manufacture of pharmaceutically active substances or corresponding intermediates.

Process for the preparation for 4,5-diamino shikimic acid derivatives

A catalytic process for the manufacture of optically active compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are alkyl, which is optionally interrupted by an O atom in a position other than the .alpha.-or .beta.-position, or optionally substituted benzyl,

Process for the preparation of optically active compounds

The invention relates to a novel process for producing a compound having the formula ##STR1## wherein R.sup.1, R.sup.2 and X are described herein, via corresponding .beta.-keto- and .beta.-hydroxy-.delta.-lactones, as well as novel intermediates which occur in the process.

Production of oxetanones

The invention relates to a novel process for producing a compound having the formula ##STR1## wherein R.sup.1, R.sup.2 and X are described herein, via wherein R corresponding .beta.-keto- and .beta.-hydroxy-.delta.-lactones, as well as novel intermediates which occur in the process.

Methyl 4-dimethylamino-3,5-dimethoxybenzoate, an intermediate in the preparation of the antibacterially active aditoprim, is obtained from 4-amino-3,5-dibromobenzoic acid by replacement of the bromine atoms by methoxy groups and subsequent methylation.

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Reinach, Switzerland

Martin Karpf