Enantioselective process for the preparation of levobunolol

Details Enantioselective process for the preparation of levobunolol Enantioselective process for the preparation of levobunolol

C - Chemistry, Metallurgy

07

C

C07C 217/74 (2006.01) C07C 213/00 (2006.01) C07C 213/04 (2006.01) C07C 217/36 (2006.01)

Patent

CA 2119052

The invention relates to a new, industrially advantageous, process for the preparation of the known beta-adrenergic blocking agent levobunolol, not requiring resolution of racemic bunolol, based on the enantioselective synthesis of an oxiranic intermediate which is then reacted with tert-butylamine. The process of this invention consists of reacting 5-hydroxy-3,4-dihydro-1(2H)-naphthalenone with (R)-(-)epichlor-hydrine in an aprotic solvent in the presence of a strong base at a temperature of over 90°C, thus obtaining the intermediate chiral oxirane (S)-5-(2,3-epoxypropoxy)-3,4-dihydro-1-(2H) --naphthalenone with more than 95% optical purity, and then, the intermediate chiral oxirane is reacted with tert-butylamine.

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