A chromatography-free synthesis of racemic salbutamol hemisulfate
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.
Vanoost, Agathe,Petit, Laurent
(2020/06/30)
A PROCESS FOR THE PREPARATION OF OPTICALLY PURE R (-) SALBUTAMOL AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS
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.
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Page/Page column 11
(2008/06/13)
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