Lonza Ag

Lonza Inc.

Polypeptide Laboratories Holding (ppl) Ab

Oleg Werbitzky

Stéphane Varray

Ulrich Daum

Rachel Bregy

Matthieu Giraud

Carsten Meininghaus

Corinne Wenger

Nicole Studer

Jasmine Schnidrig

Anne-Sophie Droz

Walter Brieden

Alfons Baiker

Yves Guggisberg

Christine Bernegger-Egli

Frank Brux

Tamas Mallat

Philipp Studer

Achim Fischer

Jean Paul Roduit

Thomas Zeiter

Etienne Heinzmann

A novel method for synthesizing a Hirulog peptide is devised.

Method for solid phase peptide synthesis

A new method of synthesizing GLP-1 peptide is devised.

Synthesis of glucagon-like peptide

A novel compound of formula I is devised. 

On-resin peptide cyclization

Method for producing (1R,4S)-2-azabicyclo&lsqb;2.2.1&rsqb;-hept-5-en-3-on derivatives

Bicyclic amidines, process for their preparation, and their use as catalyst

Process for the preparation of amines

The process for the preparation of bicyclic amidines of the general formula:

A process for the production of 2-chloro-5-chloromethylpyridine of the formula: ##STR1## starting from 6-hydroxynicotinic acid of the formula: ##STR2## In this way 6-hydroxynicotinic acid is reacted with an acid chloride to 6-hydroxynicotinoyl chloride of the formula: ##STR3## The latter is then catalytically hydrogenated with hydrogen to 6-hydroxy-5-hydroxymethylpyridine of the formula: ##STR4## The latter is then catalytically hydrogenated with hydrogen to 2-hydroxy-5-hydroxymethylpyridine of the formula: ##STR5## which is then chlorinated to the end product according to formula I.

Process for the production of 2-chloro-5-chloromethyl-pyridine

2-Amino-4,5,3',4'-tetramethoxybenzophenone of the formula: ##STR1## is prepared by mononitration of 3,3',4,4'-tetramethyoxybenzophenone using nitric acid in the presence of acetic acid, and subsequent reduction of the nitro group. The compound is an intermediate in the synthesis of active ingredients against rheumatoid arthritis.

Process for the preparation of 2-amino-4,5,3',4'-tetramethoxybenzophenone

The process for the preparation of bicyclic amidines of the general formula: ##STR1## wherein A is selected from the group consisting of --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --, --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --CR.sup.7 R.sup.8 -- and --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --CR.sup.7 R.sup.8 --CR.sup.9 R.sup.10 --, wherein the substituents in A are in each case numbered starting from the nitrogen atom, and B is selected from the group consisting of --CR.sup.11 R.sup.12 --CR.sup.13 R.sup.14 --, --CR.sup.11 R.sup.12 --CR.sup.15 R.sup.16 --CR.sup.13 R.sup.14 -- and --CR.sup.11 R.sup.12 --CR.sup.15 R.sup.16 --CR.sup.17 R.sup.18 --CR.sup.13 R.sup.14 --, and R.sup.1, R.sup.2 and R.sup.11 to R.sup.14 are, in each case independently of one another, hydrogen, C.sub.1 -C.sub.4 -alkyl, aryl, or are C.sub.1 -C.sub.4 -alkyl which is substituted with hydroxyl, amino, C.sub.1 -C.sub.4 -alkylamino or mercapto, and R.sup.3 to R.sup.10 and R.sup.15 to R.sup.18 are, in each case independently of one another, hydrogen, C.sub.1 -C.sub.4 -alkyl, aryl, hydroxyl, amino, C.sub.1 -C.sub.4 -alkylamino or mercapto, or are C.sub.1 -C.sub.4 -alkyl which is substituted with hydroxyl, amino, C.sub.1 -C.sub.4 -alkylamino or mercapto. The process includes heating (reacting) a lactone of the general formula: ##STR2## wherein A is as defined above, to at least 150.degree. C. together with an at least equimolar quantity of an amine of the general formula:

Bicyclic amidines, process for their preparation, and their use as

Process for preparing optically active

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Veyras, Switzerland

Oleg Werbitzky