Practical and scalable synthesis of beclomethasone dipropionate.

Beclomethasone dipropionate (1) is a synthetic corticosteroid with anti-inflammatory, antipruritic, and anti-allergy properties. It is widely used to treat asthma, allergic rhinitis, and dermatoses. However, existing synthetic routes to this active pharmaceutical ingredient (API) contain steps resulting in low and/or inconsistent yields, and use obsolete reagents. Such inconsistencies coupled with a lack of reliable experimental data makes laboratory-scale and large-scale synthesis of this API difficult and time-consuming. In this paper, we report a practical and scalable approach to synthesize 1 from the readily available steroidal intermediate, 16ß-methyl epoxide (3, DB-11). A gram-scale to kilogram-scale synthesis of 1 was achieved with 82% yield, using a cost-effective and scalable methodology. Selective propionylation of the hydroxyl groups at C17 and C21 demonstrate the fact that this approach can be conveniently implemented in fine chemical industries.

An efficient and high-yielding method for extraction and purification of linamarin from Cassava; in vitro biological evaluation.

During the last three decades, studies of linamarin extracted from cassava have received increased attention due to the presence of high cyanogenic compounds in these extracts. The methods that are utilized to isolate linamarin are either tedious or use acidic conditions resulting in poor yields. In this study, a novel cryocooled method of extraction has been developed to isolate linamarin from Cassava root peel. Approximately 18 g of linamarin was isolated from 1 kg of fresh Cassava root peel, which is the highest amount reported to date. Linamarin was fully characterized using NMR, IR and LCMS. The anti-cancer properties of pure linamarin and Cassava crude extract were evaluated by a comprehensive cytotoxic assay, using MCF-7, HepG2, NCI H-292, AN3CA and MRC-5 cell lines. The crude extract showed higher cytotoxicity compared to pure linamarin. The results of the biological evaluation are comparable to other reported studies in the literature.