324000-05-7Relevant articles and documents
Preparation method of salbutamol sulfate
-
, (2021/07/17)
The invention provides a preparation method of salbutamol sulfate, and relates to the technical field of chemical synthesis. The preparation method of salbutamol sulfate comprises the following steps: (a) carrying out reaction on salicylic acid and a tert-butyl amino acetyl halogenating reagent under the action of a chlorinating agent to generate an intermediate 1; (b) reacting the intermediate 1 under the action of Lewis acid to generate an intermediate 2; (c) reacting the intermediate 2 under the action of an acid reagent to generate an intermediate 3; (d) reacting the intermediate 3 with a reducing agent under the action of a catalyst to generate salbutamol; and (e) reacting salbutamol with sulfuric acid to generate salbutamol sulfate. The raw materials are simple and easy to obtain, the reaction condition is mild, the reaction operation is simple, the reaction process is easier to control, and the safety coefficient is high; used raw materials, solvents and the like are environment-friendly; and the yield and purity of salbutamol sulfate are high, and a process route capable of industrially producing a product with higher quality is provided.
Preparation method of salbutamol sulfate
-
Paragraph 0004, (2020/09/16)
The invention discloses a preparation method of salbutamol sulfate, and relates to a compound shown as a formula V. The related reaction type is simple, the used raw materials are cheap and easy to obtain, the yield is high, the environmental protection pressure is small, and the method is suitable for industrial production.
A chromatography-free synthesis of racemic salbutamol hemisulfate
Vanoost, Agathe,Petit, Laurent
, (2020/06/30)
Our efforts to achieve an efficient synthesis of racemic salbutamol hemisulfate are described. The selected chemical route starts from commodity chemicals and allows the generation of salbutamol hemisulfate in 5 steps and 44% overall yield without any purification by column chromatography. The reaction sequence has been optimized to provide the title compound using robust procedures. Emphasis on reproducibility and experimental simplicity drove the work described herein.
Predictability of enantiomeric chromatographic behavior on various chiral stationary phases using typical reversed phase modeling software
Wagdy, Hebatallah A.,Hanafi, Rasha S.,El-Nashar, Rasha M.,Aboul-Enein, Hassan Y.
, p. 506 - 513 (2013/09/12)
Pharmaceutical companies worldwide tend to apply chiral chromatographic separation techniques in their mass production strategy rather than asymmetric synthesis. The present work aims to investigate the predictability of chromatographic behavior of enantiomers using DryLab HPLC method development software, which is typically used to predict the effect of changing various chromatographic parameters on resolution in the reversed phase mode. Three different types of chiral stationary phases were tested for predictability: macrocyclic antibiotics-based columns (Chirobiotic V and T), polysaccharide-based chiral column (Chiralpak AD-RH), and protein-based chiral column (Ultron ES-OVM). Preliminary basic runs were implemented, then exported to DryLab after peak tracking was accomplished. Prediction of the effect of % organic mobile phase on separation was possible for separations on Chirobiotic V for several probes: racemic propranolol with 97.80% accuracy; mixture of racemates of propranolol and terbutaline sulphate, as well as, racemates of propranolol and salbutamol sulphate with average 90.46% accuracy for the effect of percent organic mobile phase and average 98.39% for the effect of pH; and racemic warfarin with 93.45% accuracy for the effect of percent organic mobile phase and average 99.64% for the effect of pH. It can be concluded that Chirobiotic V reversed phase retention mechanism follows the solvophobic theory. 2013 Wiley Periodicals, Inc.
PROCESS FOR THE PREPARATION OF OPTICALLY PURE R (-) SALBUTAMOL AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS
-
Page/Page column 4, (2010/08/18)
A process for the preparation of optically pure R (?) salbutamol of formula (6) and its pharmaceutically acceptable salts by using a (+) 4-nitro tartranilic acid as the resolving agent and a binary solvent system comprising alkyl acetate and C1 /sub
A PROCESS FOR THE PREPARATION OF OPTICALLY PURE R (-) SALBUTAMOL AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS
-
Page/Page column 10, (2008/06/13)
A process for the preparation of optically pure R (-) salbutamol of formula (6) and its pharmaceutically acceptable salts by using a (+) 4-nitro tartranilic acid as the resolving agent and a binary solvent system comprising alkyl acetate and C1 to C4 branched or normal chain alcohol for dissolution of the racemic mixture and resolving agent and purification of the 4-nitro tartranilic acid salt of R (-) salbutamol. 4-nitro tartranilic acid salt of R (-) salbutamol is converted into formic acid salt of R(-) 4-benzyl salbutamol followed by basification and debenzylation to form optically pure R(-) salbutamol. Optically pure (R) -salbutamol is obtained in good yield and high purity. The optically pure R(-) salbutamol is optionally converted into pharmaceutically acceptable salts.
Process for obtaining the R-enantiomer of salbutamol
-
Page/Page column 13, (2008/12/06)
The present invention relates to a process for obtaining the R-enantiomer of salbutamol from a mixture of the enantiomers of salbutamol by a crystallization of said R-enantiomer as its salt with R-ibuprofen from a solution or slurry of a mixture of the enantiomers of salbutamol.
Process for the enantiomeric enrichment of salbutamol and salbutamol precursors
-
Page/Page column 10, (2008/06/13)
The present invention relates to a process for the enantiomeric enrichment of salbutamol and salbutamol precursors and the acid-addition salts thereof: where R is hydrogen or benzyl, R' is hydrogen or benzyl and X is CH2OH or COO-C1-C4-alkyl the process comprising the crystallization of a compound of the formula I in the form of its acid-addition salt with an achiral carboxylic acid A that has at least three carbon atoms and a solubility of less than 50 g/l in water at pH 3, 20°C and 1013 mbar, from a solution containing a mixture of the enantiomers of the compound of formula I and the achiral carboxylic acid A in the presence of seed crystals of the desired enantiomer of the compound of formula I or the acid addition salt thereof, whereby the enantiomerically enriched acid-addition salt of the compound of formula I is obtained.
Enantiomeric resolution of albuterol sulfate by preferential crystallization
Palacios, Sara M.,Palacio, Marcela A.
, p. 1170 - 1175 (2008/02/08)
Albuterol is a β2-adrenoceptor agonist prescribed for the treatment of bronchial asthma; it exists as a racemate and its bronchodilator activity resides in the (R)-isomer or levalbuterol. The aim of this study was to determine a methodology that would separate the enantiomers of albuterol by preferential crystallization after a conglomerate is identified within its derivatives. We found that albuterol sulfate behaves as a conglomerate showing the characteristic αx-value = 2 (mole fraction solubility ratio of racemate vs enantiomer), the V-shaped ternary phase diagram and the preferential crystallization by seeding with the pure enantiomer. On the basis of these characteristics, we separated the enantiomers by entrainment, and crystallizing out a saturated methanolic solution of albuterol sulfate at 15 °C.
INHALABLE DRUG
-
Page/Page column 14-34, (2008/06/13)
A process for preparation of particles of an inhalable drug is described. The process comprises combining a first liquid and a second liquid in a region of high shear, whereby the first liquid and the second liquid interact to form the particles of the dr
