Perspective on Solvent Use in the Pharmaceutical Industry

Constable, David J. C.; Jimenez-Gonzalez, ‡ and Conchita; Henderson, Richard K.

doi:10.1021/op060170h

Cited by 623 publications

(464 citation statements)

References 18 publications

Supporting

Mentioning

454

Contrasting

Unclassified

Order By: Relevance

“…From a careful assessment of many of the synthetic routes to chemical products, solvents have been found to be one of the biggest mass contributors [45], as the use of solvents can lead to higher yields and thus, an improved environmental performance. This is particularly the case in the fine chemicals and pharmaceutical sectors, where the solvents typically contribute 80% to 90% of the mass intensity of a process [46].…”

Section: Si and Wimentioning

confidence: 99%

Application of environmental and economic metrics to guide the development of biocatalytic processes

Lima-Ramos¹,

Tufvesson²,

Woodley³

2014

Green Processing and Synthesis

View full text Add to dashboard Cite

Abstract:The increasing industrial interest in biocatalytic processes is predominantly driven by the need for selective chemistry, with high reaction yield (Y reaction ) and few side reactions, as well as the need for optically pure chiral molecules (in particularly in the pharmaceutical industry). Interestingly, it is often argued that the mild conditions frequently used in biocatalytic reactions (ambient temperature and pressure, neutral pH and aqueous-based media) automatically lead to environmentally-friendly and cost-effective production processes. However, such a conclusion is not justified without the use of adequate tools to evaluate the performance of a process, in particular during process development. Nevertheless, at the early development stage, evaluation of biocatalytic processes is not a trivial task, not only due to the lack of data, but also because at this stage many of the biocatalytic processes are not yet fully optimized. Hence, in this paper we propose the use of a range of tools which can be used to guide process development, research tasks and support decision-making. Three sets of metrics are identified, each for use at different stages of process development (route selection, early development and late development), each with different objectives.

show abstract

Section: Si and Wimentioning

confidence: 99%

Application of environmental and economic metrics to guide the development of biocatalytic processes

Lima-Ramos¹,

Tufvesson²,

Woodley³

2014

Green Processing and Synthesis

View full text Add to dashboard Cite

show abstract

“…Constable et al [6] have previously reported that 80-90 % of the waste mass generated by typical batch chemical operations will often come from the solvent. More recently, estimates from the American Chemical Society Green Chemistry Institute Pharmaceutical Roundtable (ACS-GCIPR) have shown 56 % of the mass needed to produce 1 kg of an active pharmaceutical ingredient (API) will come from solvent [7].…”

Section: Introductionmentioning

confidence: 99%

Greener solvents for solid-phase organic synthesis

Lawrenson

2017

Pure and Applied Chemistry

View full text Add to dashboard Cite

Solid-phase organic synthesis is an essential method for the rapid synthesis of complex biological structures and libraries of small organic molecules. However, it is often associated with the use of large quantities of problematic solvents for the removal of excess reagents and reaction by-products. Given that solvent will often be the biggest contributor to waste generated in the average pharmaceutical/fine-chemical process, its exchange for a more desirable alternative often presents the biggest gains in terms of reducing environmental impact. This review aims to explore recent approaches to performing solid-phase organic synthesis, and associated solid-phase peptide synthesis, in neoteric solvents and reaction media that present greener alternatives.

show abstract

“…16 Considerando todos os aspectos das transformações químicas sustentáveis, tais como economia de átomos, catálise e eficiência energética, entre outros, o meio reacional tem papel muito importante. De acordo com Constable et al, 17 o solvente da reação representa até 80% do total de toda a massa de materiais para os processos químicos de produção de Ingredientes Farmacêuticos Ativos (Active Pharmaceutical Ingredient, API). Diante disso, grandes indústrias farmacêuticas como a Pfizer, 18 a GSK, 19 e a Sanofi 20 desenvolveram recentemente guias de seleção de solventes para processos químicos aplicados à síntese de APIs.…”

Section: Introductionunclassified