Synthesis of the β2-Agonist Tulobuterol and Its Metabolite 4-Hydroxytulobuterol
Abstract: Alternative methods have been developed for the synthesis of theβ2-agonist tulobuterol and its metabolite4-hydroxytulobuterol with a similar activity. The proposed procedures utilizeavailable reagents, and the key stage in the synthesis is the formation ofintermediate oxirane according to the Corey–Chaykovsky reaction, followed byopening of the oxirane ring by the action of excess tert-butylamine. In the synthesis of 4-hydroxytulobuterol, thehydroxy group was protected by benzylation, and the protecting group was removedin the final stage by hydrogenation over carbon-supported palladium.
Burdeinyi, M. L.,Glushkova, M. A.,Popkov, S. V.
p. 390 - 394
(2020/04/27)
Optically active benzyl alcohol compound and pharmaceutical composition
A levo-rotatory enantiomer of benzyl alcohol compound represented by the following formula (I): wherein .C represents an asymmetric carbon atom; a pharmacologically acceptable salt of the compound; and a method for preparing the enantiomer is disclosed. Also disclosed are methods for ralaxing uterine smooth muscle and bladder smooth muscle comprising administering the levo-rotatory enantiomer. Further disclosed is a pharmaceutical composition for the treatment of premature labor or incontinence of urine comprising an effective amount of the levo-rotatory enantiomer together with a pharmaceutically acceptable carrier or coating. Lastly disclosed are methods for the treatment of premature labor or incontinence of urine comprising the steps of determining that a mammal has one of these illnesses and administering the levo-rotatory enantiomer to the mammal.
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(2008/06/13)
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