Formoterol process
AssigneeSepracor Inc.
InventorsYun Gao, Robert Hett, Kevin Q. Fang, Stephen A. Wald, Martin P. Redmon, Chris Hugh Senanayake
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Abstract
A method is disclosed for the preparation of optically pure isomers of formoterol by the reaction of an optically pure 4-benzyloxy-3-formamidostyrene oxide with an optically pure 4-methoxy-.alpha.-methyl-N-(phenylmethyl)benzeneethanamine followed by debenzylation. Useful intermediates in the process are also disclosed, as are the novel L-tartrate salt of R,R-formoterol and pharmaceutical compositions thereof.
Claims10
Crystalline R,R-formoterol L-(+)-tartrate.
Solid R,R-formoterol L-(+)-tartrate having a melting point greater than 179.degree. C.
A polymorph of R,R-formoterol L-(+)-tartrate having a transition point in differential scanning calorimetry of about 193.degree. C. and a solubility in water at 25.degree. C. of about 15 mg/mL.
A polymorph of R,R-formoterol L-(+)-tartrate having a transition point in differential scanning calorimetry of about 180.degree. C. and a solubility in water at 25.degree. C. of greater than 25 mg/mL.
A pharmaceutical composition comprising R,R-formoterol L-(+)-tartrate and a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.