24085-07-2Relevant articles and documents
Preparation method of salbutamol intermediate V hydrochloride
-
Paragraph 0023; 0024, (2018/11/03)
Salbutamol is a beta receptor stimulant. In the conventional preparation technology of salbutamol, reference listed drug technology is taken as the main research content; in the reference listed drugtechnology, p-Hydroxyacetophenone is taken as an initial
Preparation method of leverbuterol and its salt
-
Paragraph 0019; 0020; 0021; 0022; 0023, (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.
Synthesis of the β2 Agonist (R)-Salmeterol Using a Sequence of Supported Reagents and Scavenging Agents
Bream, Robert N.,Ley, Steven V.,Procopiou, Panayiotis A.
, p. 3793 - 3796 (2007/10/03)
(Matrix Presented) The enantioselective synthesis of (R)-salmeterol has been achieved by using a sequence of supported reagents and sequestering agents. The saligenin core was installed by a regiospecific alkylation and a chiral auxiliary approach was employed to introduce the desired stereochemistry via a diastereoselective reduction.