Continuous flow process for preparing budesonide

• Published in: Journal of flow chemistry Vol. 12; no. 2; pp. 237 - 246
• Main Authors: Phull, Manjinder Singh, Jadav, Surender Singh, Bohara, Chander Singh, Gundla, Rambabu, Mainkar, Prathama S
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 2022
• Subjects: Chemistry; Chemistry and Materials Science; Chemistry/Food Science; Green Chemistry; Industrial Chemistry/Chemical Engineering; Inorganic Chemistry; Nanochemistry; Organic Chemistry; Epimers; Budesonide; Flow reactor; Glucocorticosteroid; Isomeric ratio
• ISSN: 2062-249X; 2063-0212
• DOI: 10.1007/s41981-022-00221-5

Budesonide, a glucocorticosteroid, is used as anti-asthmatic drug that became generic in 2019. Existing preparation methods of budesonide require utilization of corrosive acids and involve expensive purification process. Thus, a new cost-effective continuous flow process for the synthesis of budesonide which belongs to the class of 16,17 acetals of pregnane core, is discussed in the present research findings. Flow reactor parameters such as flow rate, temperature, residence time, solution volumes, anti-solvents and reactor frequency are subjected to investigation on the preparation of molar ratio of budesonide epimers. Further, the suitable parameters entail for obtaining the desired molar ratio of epimers. In another aspect, particle size optimization studies are also performed to get the desired budesonide solid product. A continuous flow process for preparation of budesonide is identified from the present research investigation which can be readily transferred to industrial scale up. Graphical abstract