Sandoz Ag

Sandoz Gmbh

Wolfgang Felzmann

Birgit Endl

Hannes Lengauer

Thorsten Wilhelm

Martin Langner

Michael Fischer

Niklas Schone

Kathrin Hoeferl-Prantz

Ronny Huetz

David Benito-Garagorri

The present invention relates to a highly convergent method for the synthesis and purification of ceftolozane and intermediates starting from 7-aminocephaiosporanic acid (7-ACA).

Process for preparing ceftolozane from 7-aminocephalosporanic acid (7-ACA)

The present invention relates to the preparation of compounds, in particular to the preparation of compounds which may be used as intermediates for the preparation of antibiotics, preferably carbapenem antibiotics, more preferably ertapenem, and salts thereof.

Preparation of ertapenem intermediates

The invention relates to synthetic routes for preparing telaprevir and boceprevir, and its intermediates as well as peptides other than telaprevir. The synthetic routes are based on a Mukaiyama aldol addition reaction of a silyl enol ether or an enolate with an imine. The invention also refers to novel intermediates for preparing telaprevir/boceprevir or other peptides.

Synthesis of telaprevir and boceprevir, or pharmaceutically acceptable salts or solvates as well as intermediate products thereof including &#x3b2;-amino acids prepared via Mukaiyama aldol addition

The invention refers to the selective acylation of Rapamycin at the 42-position (I) with an acylating agent of the formula (II) wherein Rand Rare the same or different, individually the rest of an acetal, especially tetrahydropyran, or of a carbonate or the rest of a silyl ether or taken together are the rest of a boronate, an acetal or ketal. 

Regioselective acylation of rapamycin at the C-42 position

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Kundl, Austria

Wolfgang Felzmann