Lek Pharmaceuticals D.d.

Peter Mrak

Gregor Kopitar

Zdenko Casar

Matej Oslaj

Tomaz Mesar

Hrvoje Petkovic

Gregor Kosec

Stefan Fujs

Jerome Cluzeau

Stefan Starcevic

Enej Kuscer

Tadeja Zohar

The present invention relates to a process for preparing &#x25a1;-aminobutyryl substituted 5,6,7,8-tetrahydro[1,4]diazolo[4,3-&#x3b1;]pyrazin-7-yl compounds.

Synthetic route for the preparation of &#x3b2;-aminobutyryl substituted 5,6,7,8-tetrahydro[1,4]diazolo[4,3-alpha ]pyrazin-7-yl compounds

Genetically modified strains of() can be used for an improved fermentation process for the preparation of tacrolimus or a salt or derivative thereof by cultivation of these genetically modified strains. Novel genes allowing biosynthesis of allylmalonyl-CoA can be used for polyketide production with allylmalonyl extender unit.

Process for preparation of tacrolimus

The process for the synthesis of statins featuring the use of an early intermediate (4R,6S)-6-(dialkoxymethyl)tetrahydro-2H-pyran-2,4-diol which already possesses the desired stereochemistry corresponding to the final statin.

Synthesis of statins

The present invention relates to ((2S,4R)-4,6-dihydroxytetrahydro-2H-pyran-2-yl)methyl carboxylates and a process for the production thereof. Furthermore, the present invention relates to a process for the production of statins and in particular of Rosuvastatin and derivates thereof, wherein the above mentioned compounds are used as intermediates.

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Ljubljana, Slovenia

Peter Mrak