Green Chemistry in Process Research and Development in Pharmaceutical Industry

Autor:	Masanori Nisiwaki
Rok vydání:	2003
Předmět:	Green chemistry Active ingredient Chemistry business.industry Process (engineering) Scale (chemistry) Organic Chemistry General Medicine Work in process Environmentally friendly Zenarestat Organic chemistry Biochemical engineering business Pharmaceutical industry
Zdroj:	Journal of Synthetic Organic Chemistry, Japan. 61:464-471
ISSN:	1883-6526 0037-9980
DOI:	10.5059/yukigoseikyokaishi.61.464
Popis:	Recently, green chemistry (GC) plays an important role for manufacturing active pharmaceutical ingredients (APIs) at pharmaceutical companies. For example, large amount of aluminum waste was originally involved and dichloromethane used as a solvent in the process of a new anticholinergic agent, Vamicamide (FK 176), useful for the treatment of urinary incontinence. Non-selective and tedious procedures for alkylation of quinazoline nucleous were used on a laboratory scale in the process of a novel aldose reductase inhibitor, Zenarestat (FK 366) developed for the remedy of diabetic complications. These problems must be excluded before realizing a truly efficient process on a large scale. New process involved much less amount of waste in the case of Vamicamide, and utilized regioselective alkylation reaction for Zenarestat. As a result, E-factor and reaction mass efficiency (RME) were dramatically improved. Herein, we report our efforts leading to an efficient, practical and environmentally friendly process amenable to a large scale synthesis.
Databáze:	OpenAIRE
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