Dsm Sinochem Pharmaceuticals Netherlands B.v.

Dsm N.v.

Gist-brocades B.v.

Gist-brocades N.v.

Centrient Pharmaceuticals Netherlands B.v.

Dsm Sinochem Pharmaceuticals

Robertus Mattheus De Pater

Johannes Wilhelmus Lambers

Dhiredj Chandre Jagesar

Mieke Sibeijn

Jan Verweij

Ben De Lange

Peter Philip Lankhorst

Hein Simon Koger

Thomas Van Der Does

Piotr Wnukowski

Neeraj Tewari

Jan W Smeets

Burhan Özalp

Mieke Sibeyn

Roop Singh Yadav

Adrianus Antonius Cornelius Van Wijk

Aad Johannes Bouman

Cornelis Frederik Purmer

Paulus Bernardus Maria Groen

The present invention relates to a process for acylating cyclic peptides bearing an amino group and to the application of said process in the preparation of anidulafungin and micafungin.

Method for acylating a cyclic peptide

The present invention relates to a method for isolating caspofungin and to a novel crystalline form of caspofungin diacetate thus obtained.

Method for isolating caspofungin

The present invention relates to a novel cyclohexapeptide, to a method for the preparation of said cyclohexapeptide and to the use of said cyclohexapeptide.

Cyclohexapeptide

The present invention relates to a method for isolating acyclohexapeptide and to a novel crystalline form of caspofungin diacetate thus obtained.

Method for isolating a cyclohexapeptide

The present invention relates to a method for preparing cyclopeptides by means of protection with a substituted boronic acid. The present invention also discloses novel boronate esters of cyclopeptides of general formula (8). 

Method for the preparation of cyclopeptides

The present invention relates to a method for the purification of cyclopeptides of general formula (3) by means of a silicate. 

Purification of caspofungin intermediates

The present invention relates to a salt of a carboxylic acid with a diamine such as 2,2'-(ethylenedioxy)diethyl amine, 3,3&#x2032;-(ethylenedioxy)dipropyl amine and 2,2&#x2032;-oxybis(ethylamine) and a method of preparing such salts. Preferably the carboxylic acid is a fermentation product such as clavulanic acid, mycophenolic acid or pravastatin.

Diamine salts of carboxylic acids

The present invention provides a method for the preparation of mycophenolate mofetil wherein mycophenolic acid or an amine salt of mycophenolic acid is esterified with 2-morpholinoethanol, the resulting mixture is extracted into water at a pH-value between 1.0 and 3.0, and mycophenolate mofetil is back-extracted in a water-immiscible solvent at a pH-value between 3.0 and 5.0.

Method for the purification of mycophenolate mofetil

A process for the isolation of crystalline carotenoid compound from microbial biomass comprising disrupting the microbial cell walls, separating cellular debris from the carotenoid-containing residue, washing one member of the group consisting of the microbial biomass, the disrupted cell mass and the carotenoid-containing reside with a solvent to remove lipid, suspending the obtained carotenoid crystals in water to float the crystals, recovering the crystals and, optionally, further purifying the crystals which avoids the use of large amounts of solvent of carotenoid extraction process.

Isolation of carotenoid crystals from microbial biomass

The invention provides a simple and selective method for the deacylation of 4-acylated statins during the preparation of statins from a fermentation broth, more specifically a reduction of impurities from the process, by increasing the pH of the fermentation broth.

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Delft, Netherlands

Robertus Mattheus De Pater