39235-61-5Relevant articles and documents
Preparation method of leverbuterol and its salt
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Paragraph 0041; 0042; 0043; 0044; 0045, (2017/06/02)
The invention provides a method for cheap and effective preparation of leverbuterol in industry. The method consists of: taking protected 4-hydroxy-3-hydroxymethyl acetophenone as the raw material to react with bromine to generate acyl or alkyl protected 4-hydroxy-3-hydroxymethyl bromoacetophenone, under in the presence of (1R, 2S)-(+)-indanol as a catalyst, using borane to conduct chiral reduction on carbonyl in the structural formula to obtain R configuration acyl or alkyl protected 4-hydroxy-3-hydroxymethyl alpha bromo phenethyl alcohol, then carrying out reaction with tert-butylamine to generate acyl or alkyl protected 4-hydroxy-3-hydroxymethyl phenylaminoethanol, and finally removing the acyl protecting group to obtain leverbuterol free alkali, and letting the free alkali and acid form a salt. The finished product has optical purity up to 99.9%, and no other chiral resolution way is needed for purification.