Preparation of enantiopure antimalarial agent (+)-mefloquine

• Research unit: INNOSUISSE
• Project number: 15523.1 PFLS-LS

Short description (German)

Preparation of enantiopure antimalarial agent (+)-mefloquine

Short description (English)

Preparation of enantiopure antimalarial agent (+)-mefloquine

Abstract (German)

Chiral amines are key components of pharmaceuticals but can be difficult, enviornmentally unfriendly, and|expensive to prepare. An excellent example of this problem is mefloquine, an anti-malerial drug currently|available only as a racemic mixture despite the fact that the (+)-enantiomer exhibits the desired activity while the side effects are associated with the (-)-enantiomer. This project will develop a new technology for separating the enantiomers of chiral amines from their mixtures on a kilogram scale. Working with Roche, this technology will be scaled up and used to prepare several hundred grams of enantiopure (+)-mefloquine, a quantity sufficient for early stage clinical trials.

Abstract (English)

Chiral amines are key components of pharmaceuticals but can be difficult, enviornmentally unfriendly, and|expensive to prepare. An excellent example of this problem is mefloquine, an anti-malerial drug currently|available only as a racemic mixture despite the fact that the (+)-enantiomer exhibits the desired activity while the side effects are associated with the (-)-enantiomer. This project will develop a new technology for separating the enantiomers of chiral amines from their mixtures on a kilogram scale. Working with Roche, this technology will be scaled up and used to prepare several hundred grams of enantiopure (+)-mefloquine, a quantity sufficient for early stage clinical trials.