62932-94-9Relevant articles and documents
Synthesis method of salbutamol sulfate intermediate
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Paragraph 0028; 0033-0036, (2021/05/05)
The invention discloses a synthesis method of a salbutamol sulfate intermediate, which comprises the following steps: by taking salicylaldehyde as a raw material, carrying out three-step reaction of Friedel-Crafts acylation, reduction, propylidene protection and N alkylation, and obtaining the target product salbutamol intermediate with the reaction yield of more than 60% in each step. The synthesis method of the salbutamol sulfate intermediate has the advantages of few reaction steps, simple post-treatment and high product purity.
Method for synthesizing Vilanterol intermediate in mixed solvent
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Paragraph 0012; 0021-0032, (2019/04/17)
The invention discloses a method for synthesizing a Vilanterol intermediate in a mixed solvent, and belongs to the field of drug synthesis. According to the method, 5-bromoacetyl-2-hydroxybenzaldehydeis reduced by sodium borohydride in the mixed solvent to obtain 2-bromo-1-[4-hydroxy-3-(hydroxymethyl) phenyl] ethyl-1-ketone. Reaction selectivity and yield are improved, post-treatment is simple, and the method is suitable for industrial production.
Levalbuterol intermediate and synthetic method of levalbuterol hydrochloride
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Paragraph 0045; 0046; 0047; 0048, (2017/08/25)
The invention provides a levalbuterol intermediate and a levalbuterol hydrochloride synthesis method, and relates to a levalbuterol intermediate and a method for preparing levalbuterol hydrochloride from the intermediate. The method comprises steps as follows: 2-halogenate-1-(2,2-dimelthyl-4-hydrogen-benzo [d][1,3] dioxane)-butanone and organic amine have a Hoffman alkylation reaction to prepare a compound in the formula 2, the structural formula of the compound is shown in the specification, and the compound in the formula 2 is subjected to a reduction reaction, optically pure organic acid resolution and deprotection by hydrochloric acid to obtain levalbuterol hydrochloride. The method does not need processes of protection or deprotection and the like of hydroxyl groups on a benzene ring, protection, deprotection and purification processes are reduced, the synthesis route is short, operation is simple, meanwhile, borane-thioether does not need to be used as a reduction agent, and safety and environmental protection are realized.
Hybrids consisting of the pharmacophores of salmeterol and roflumilast or phthalazinone: Dual β2-adrenoceptor agonists-PDE4 inhibitors for the treatment of COPD
Liu, Anqiu,Huang, Ling,Wang, Zhiren,Luo, Zonghua,Mao, Fei,Shan, Wenjun,Xie, Jiaxing,Lai, Kefang,Li, Xingshu
, p. 1548 - 1552 (2013/03/28)
A novel class of dual pharmacology bronchodilators targeting both β2-adrenoceptor and PDE4 was designed and synthesised by combining the pharmacophores of salmeterol and roflumilast or phthalazinone. All the compounds exhibited better β2-adrenoceptor agonist activities (pEC50 = 8.47-9.20) than the reference compound salmeterol (pEC50 = 8.3) and good inhibitory activity on PDE4B2 (IC 50 = 0.235-1.093 μM).
A convenient synthesis of (R)-salmeterol via Rh-catalyzed asymmetric transfer hydrogenation
Liu, Juntao,Zhou, Di,Jia, Xian,Huang, Ling,Li, Xingshu,Chan, Albert S.C.
, p. 1824 - 1828 (2008/12/22)
(R)-Salmeterol was synthesized in eight steps with salicaldehyde as the starting material. The key chiral intermediate, alcohol 5, was prepared via Rh-catalyzed asymmetric transfer hydrogenation with (S,S)-PEG-BsDPEN or (S,S)-TsDPEN ligand and sodium formate as the hydrogen donor under mild conditions.
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.
3,4-disubstituted phenylethanolaminotetralincarboxamide derivatives
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, (2008/06/13)
The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxamide derivatives represented by the general formula: STR1 (wherein A represents a lower alkylene group; B represents an amino group, a di(lower alkyl)amino group or a 3 to 7-membered alicyclic amino group which may contain an oxygen atom in the ring; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration) and pharmaceutically acceptable salts thereof, which have a selective β 2 -adrenergic receptor stimulating effect with relieved burdens on the heart such as tachycardia and are useful as an agent for the prevention of threatened abortion and premature labor, a bronchodilator and an agent for pain remission and stone removal in urolithiasis.
3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivatives
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, (2008/06/13)
PCT No. PCT/JP97/01008 Sec. 371 Date Mar. 8, 1999 Sec. 102(e) Date Mar. 8, 1999 PCT Filed Mar. 26, 1997 PCT Pub. No. WO97/35835 PCT Pub. Date Oct. 2, 1997The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivatives represented by the general formula: [wherein Q represents a vinylene group or a group represented by the general formula: -A-(CH2)m-(wherein A represents an oxygen atom or a methylene group; and m is an integer of from 1 to 6); R represents a hydrogen atom or a lower alkyl group; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration] and pharmaceutically acceptable salts thereof, which have a selective beta 2-adrenergic receptor stimulating effect with relieved burdens on the heart such as tachycardia and are useful as an agent for the prevention of threatened abortion and premature labor, a bronchodilator and an agent for pain remission and promoting stone removal in urolithiasis.