Desformoterol and process for its preparation

Details Desformoterol and process for its preparation Desformoterol and process for its preparation

1998-06-23

1999-10-12

Reamer, James H.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Nitrogen containing other than solely as a nitrogen in an...

564255, A61K 31135

Patent

active

059656220

ABSTRACT:
The (R,R)-, (S,S)-, (R,S)-, (R,S)- isomers of 3-amino-4-hydroxy-.alpha.-[[[2-(4-methoxyphenyl)-1-methylethyl]amino]methy l]-benzenemethanol (D) ##STR1## are disclosed, as well as an efficient method for their stereoselective synthesis. A method and composition are also disclosed utilizing desformoterol (D) as a bronchodilator, having high selectivity for .beta..sub.2 receptors.

REFERENCES:
Hett, R. et al., "Large-Scale Synthesis of Enantio-and Diastereomerically Pure (R,R)-Formoterol," Organic Process Research & Deveopment, vo. 2, pp. 96-99, 1998.
Hett, R. et al., Enantio-and Diastereoselective Synthesis of all Four Stereoisomers of Formoterol, Tetrahedron Letters, vol. 38, No. 7 pp. 1125-1128, 1997.

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