Basilea Pharmaceutica Ag

Studiengesellschaft Kohle Mbh

Mario Waser

Daniel Mink

Ruben Van Summeren

Harrie Vaessen

Alois Fürstner

Christina Nevado-Blàzquez

Emilie Moulin

Christophe Aïssa

The invention relates to a process for the manufacture of diastereomerically and enantiomerically enriched triazole compounds isavuconazole and ravuconazole, comprising a Reformatsky reaction between a ketone and a 2-halozincpropionate ester, followed by a resolution step, preferably an enzymatic resolution with an esterase enzyme.

Process for the manufacture of isavuconazole or ravuconazole

The invention relates to Iejimalides having the following formula (I) in which a, b, c, d, e, f, g, h, i, j, k, l, m, n, o, p are simple or double bonds, the continuous lines representing at least one simple bond, the dotted lines representing a possible bond. A double bond can be present but it is not necessary, and provided that a continuous line is also present, or a simple bond can be present if no other line is represented; m=0-20 and n1-n18=1, 2. The bonds can be used as chemotherapeutic agents for treating cancer.

Iejimalid analoga and uses thereof

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Leonding, Austria

Mario Waser