Preparation of p-chirogenic phospholanes and their use in...

Details Preparation of p-chirogenic phospholanes and their use in... Preparation of p-chirogenic phospholanes and their use in...

C - Chemistry, Metallurgy

07

F

C07F 9/6568 (2006.01) C07F 15/00 (2006.01)

Patent

CA 2561755

Materials and methods for preparing P-chirogenic monophospholanes and bisphospholanes are disclosed. The methods employ stereoselective cyclization to generate the phospholane rings followed by pyramidal inversion to access a variety of P-chirogenic phospholanes. When bound to transition metals such as rhodium, the disclosed P-chirogenic phospholanes may be used as catalysts in asymmetric synthesis of valuable pharmaceutical chemical entities, including pregabalin.

La présente invention concerne des matières et des procédés pour préparer des monophospholanes et des biphospholanes P-chirogènes. Lesdits procédés mettent en oeuvre une cyclisation stéréosélective afin de produire les noyaux de phospholane, suivie d'une inversion pyramidale permettant d'accéder à une variété de phospholanes P-chirogènes. Lorsqu'ils sont liés à des métaux de transition tels que le rhodium, les phospholanes P-chirogènes selon cette invention peuvent être utilisés comme catalyseurs dans une synthèse asymétrique d'entités chimiques pharmaceutiques importantes, notamment de prégabaline.

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