24085-07-2Relevant articles and documents
Preparation method of salbutamol intermediate V hydrochloride
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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
Preparing method of levalbuterol
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Paragraph 0082; 0083; 0084; 0085; 0086; 0087; 0088; 0089-96, (2017/04/29)
The invention provides a preparing method of levalbuterol (5) shown in the formula (5). The preparing method includes the steps that a compound shown in the formula (1) reacts with formaldehyde and acetic anhydride to obtain a compound (2) shown in the formula (2); a compound (3) shown in the formula (3) is obtained through bromination; a compound (4) shown in the formula (4) is obtained through asymmetric reduction; the compound finally reacts with tert-butylamine, and the protecting group is removed to obtain levalbuterol (5) shown in the formula (5). The preparing method is simple in path, easy to operate, mild in reaction condition, high in yield and stereoselectivity and low in industrial production, and has short steps and high practical application value and social economic benefits.
Preparation method of leverbuterol and its salt
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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.