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Report

Teaser, summary, work performed and final results

Periodic Reporting for period 1 - SpartWISE (Reinventing fine chemicals synthesis: large-scale production of sparteine from lupin beans)

Teaser

Summary

Spartax Chemicals was founded with a mission to address specific needs in the chemicals market. We aim to discover useful reagents and novel chemical transformations developed in a sustainable way and commercialise them at highly competitive prices. We have developed an innovative process for the large scale production of Sparteine, using as raw material a compound extracted from lupin processing wastewater. Historically, (-)-Sparteine has been widely employed as chiral ligand in asymmetric synthesis and co-catalyst in ring-opening polymerisation reactions and also in the development of synthetic routes of drug candidates and commercial drugs like the anticonvulsant (S)-Pregabalin.
For decades (-)-Sparteine was used as chiral ligand in asymmetric synthesis, whereas the potential of (+)-Sparteine has never been exploited due to its very low market availability and high prices. However, around the year 2010 and unexpectedly, also the (-)-Sparteine enantiomer has become scarce and very expensive. The shortage affected both academia and industry and the search for alternative synthetic methodologies and Sparteine surrogates attracted the interest of major players within the pharmaceutical industry. Despite the combined efforts these alternatives are not effective or economically viable for large scale production. The SpartWISE process was developed to address the market need for reliable sources of both enantiomers of Sparteine, and supply large amounts of pure Sparteine to academic researchers, pharmaceutical companies and CROs.
Within the chiral chemicals market, the specialty chemicals are a major driver in chemical industry. With a broad field of applications, it covers numerous sectors such as the fine chemicals, food additives, biocides and catalysts that all together are instrumental in improving todayâ€™s quality of life, health and wellbeing, while contributing for a better future.
Within this study we proposed to refine our market hypothesis and perform a thorough assessment based on the technical and financial feasibility and market potential for the large scale production and commercialisation of Sparteine.

Work performed

The starting point for the SpartWISE project was a deeper identification of our target customers, by characterising the different potential customers and elaborating a preferred customer profile.
Initial work was performed on screening different organisations that could potentially use Sparteine on their processes. However, given the secretive nature of the ongoing research programs and synthetic methodology employed in most of our target customersâ€™ organisations, an accurate identification is hard to achieve.
As such we changed our strategy in order to perform a stratification of potential customers and a complete profiling of each category. We performed a portfolio analysis that allowed us to identify the preferred markets to address, taking into consideration the idiosyncrasies of each one.
Based on this analysis we elaborated a commercialisation strategy to deploy our products to the market. To successfully implement this strategic plan, we had to incorporate a technical analysis of our production up-scaling. After a thorough examination of the production process, we concluded that even medium scale production is not viable in a laboratory setting and the initial step of the production process needs to be industrialised. Before going to multi-kilogram production, the process needs to be validated in a pilot unit to achieve at least 500 g of (-)- Sparteine in a single batch. Concomitantly, we have been establishing contacts to study the best strategy to produce these batches.
Most importantly, our patent only grants us protection in the second step of the production and in few countries. While the initial step is kept as a trade secret, for the second step there is a limited number of countries where the up-scaling process can be performed under protection.
During the feasibility study, we also evaluated the possibility of licencing the patent. However, different factors suggested that this wasnâ€™t the best option. First, the fragility of the patent in number of countries covered, which limited Spartax Chemicals to find the best available partner to these countries. Second, the origin of raw materials is kept as trade secret. And finally, since the patent only protects the second step of the process, the company is not willing to share confidential information about the initial steps that could be easily modified and performed in other countries, thus eliminating Spartaxâ€™s leverage.
In summary, we are now establishing a partnership to use a pilot production unit, in order to produce a multi-gram batch of (-)- Sparteine. Upon completion, we will be able to approach and offer the potential customers high amounts of product for their assessment. Given the methodology adopted by these companies, with well-established protocols, it is critical to fulfil their criteria for new suppliers â€“ high quality, fast response and affordable prices. As such, we are also launching a new website and presence in the social media â€“ Linkedin and Twitter â€“ to increase outreach and create brand awareness.

Final results

The SpartWISE project aims to enable the production of kg amounts of Sparteine, and deployment to the market. The use of Sparteine by different stakeholders in the chemical industry has been limited by a number of factors. Namely, the cyclic rupture of stock availability in main vendors, the worldwide price fluctuation and the lack of bulk amount suppliers. Consequently, the industry players searched for alternatives, that never fulfilled their needs nor did these alternatives performed as well as Sparteine. With the SpartWISE project we aim to revert this situation, promoting the access to unlimited amounts of Sparteine. We identified the specialty chemicals as the top market for our product. The specialty chemicals industry is a very complex and competitive sector, where products are outranked based on their performance. As such, the selection of components or reagents for manufacturing is very strict. When manufacturers and producers identify a trusty supplier, this becomes a premium choice for their processes. Our goal is to become a trustworthy brand and the first choice for companies in need of Sparteine all over the world.
In 2018 the worldâ€™s five largest specialty chemicals segments where the specialty polymers, industrial and institutional cleaners, electronic chemicals, surfactants and flavors and fragrances. Collectively, these five segments had a market share of 37% total annual specialty chemicals sales.
Sparteine as been primarly used as chiral ligand in asymmetric syntheses and co-catalyst in ring-opening polymerisation reactions and consequently, it is easy to believe that we can further expand our portfolio of applications to broader fields, once the the scale up production is finished and the brand Spartax Chemicals achieves market recognition.
On the other hand, the SpartWISE project emerged from a recycling approach, aiming to clean wastewater from lupin processing units, recovering added value products. This approach, can clearly be applied to different sectors of the food industry, following the same guidelines of the SpartWISE project, to decrease the level of contamination of food processing waste and to recover valuable chemical compounds that may represent a versatile and cheaper source of materials for the chemical industry.