- Salbutamol hydrochloride preparation method suitable for industrial production
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The invention discloses a salbutamol hydrochloride preparation method suitable for industrial production. 4-hydroxy-3-hydroxymethylacetophenone used as an initial raw material undergoes epoxy protection, oxidation, reductive amination and deprotection salification to obtain salbutamol hydrochloride. The method has the advantages of no bromination process in the whole reaction process, avoidance ofuse of high-risk reagents, small environmental pollution, low device requirements, simplicity in operation, mild reaction conditions, simplified steps, low production cost, and suitability for industrial production.
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- Preparation method of free racemic albuterol
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The invention discloses a preparation method of free racemic albuterol. The preparation method comprises the following steps: with methyl salicylate as a raw material, successively carrying out Friedel-Crafts acylation and oxidation, carrying out condensation and borate reduction in pure water with a 'one-pot' method, carrying out ester group reduction and acetonylidene protection of crude albuterol with a 'one-pot' method, and carrying out deprotection and purification to obtain the free racemic albuterol. The preparation method has the advantages of high labor efficiency, low reaction reagent cost and high yield.
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Paragraph 0049
(2018/12/13)
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- Levalbuterol intermediate and synthetic method of levalbuterol hydrochloride
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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.
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Paragraph 0057; 0058; 0059; 0060
(2017/08/25)
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- SUBSTITUTED PHENYLPHOSPHATES AS MUTUAL PRODRUGS OF STEROIDS AND β -AGONISTS FOR THE TREATMENT OF PULMONARY INFLAMMATION AND BRONCHOCONSTRICTION
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A mutual prodrug of a corticosteroid and a substituted phenylphosphate (β-agonist derivative) for formulation for delivery by aerosolization to inhibit pulmonary inflammation and bronchoconstriction is described. The mutual prodrug is preferably formulate
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Page/Page column 33-34
(2008/06/13)
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- Process for the production of optically enriched (R)- or (S)-albuterol
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A process for the production of optically enriched (R)- or (S)-albuterol or (R)- or (S)-albuterol salts by the resolution of a novel ketal derivative 2-(N-t-butylamino)-1-(+2,2-dimethyl-1,2-benzodioxin-6-yl) ethanol, with a chiral tartaric acid derivative.
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- Resolution of albuterol acetonide
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The (R)-enantiomer of albuterol has been isolated via resolution of albuterol acetonide with (2S,3S)-di-O-benzoyl- or (2S,3S)-di-O-toluoyltartaric acid. The absolute configuration of the resolved acetonide was assessed by 1H NMR analysis of its (R)-Mosher's ester, and confirmed by an X-ray crystal structure determination of the (R)-phenylethylurea derivative of the (S)-enantiomer.
- Caira, Mino R.,Hunter, Roger,Nassimbeni, Luigi R.,Stevens, Anne T.
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p. 2175 - 2189
(2007/10/03)
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