Sinocompound’s new plant in Tongling, China

When developing new drugs, it is essential to get them through the clinical trial stages quickly, with the ultimate aim of going to market to benefit those needing treatment. Unfortunately, drug discovery and development aren’t quick processes, and it takes over a decade from a medicine’s conception to market – if it makes it at all. Scientists invest substantial amounts of time and resources into research and manufacturing, to reduce costs and increase project efficiency.

One of the most significant ways to streamline the process is to invest in the drug development and early scale-up stages. It’s a remarkable expense – around two-thirds of the overall cost – but it’s necessary to bring your innovations to market as soon as possible. By optimizing this stage, you can get your project to where it needs to be, in the most time- and economically effective manner.

Unfortunately, it’s not a straightforward process. For example, you generally require novel methodologies and access to the right materials to expedite the development stage. Here we examine how working with a specialist can provide you with the necessary tools to supply your innovations to those in need, faster.

Catalyzing success

Incorporating catalytic steps into your synthesis route can bring massive benefits to your project by:

• Facilitating new reactions (such as cross couplings) to reach your final product
• Reducing associated costs
• Reducing the number of synthetic steps, speeding-up product delivery

However, introducing catalytic steps has challenges, too. Once you’ve selected the optimal catalyst from your library that enables an efficient process, you need to make sure that you can access it on scale. As there are so many ligands and catalysts available, if your preferred option isn’t widely utilized, you may not be able to obtain it in kilogram scales.

Bringing QPhos to the forefront of research

Take QPhos as an example. QPhos is a highly effective ligand in many metal-catalyzed cross-coupling reactions. From α-arylation of carbonyl compounds to late-stage C-C bond formation, QPhos shows great promise in drug discovery and development.

While QPhos has been investigated for synthesis of some biologically relevant compounds, such as an 11ββ-HSD1 inhibitor for Merck, it hasn’t been widely incorporated into screening programs as it’s simply not available in significant quantities. However, a gem like QPhos shouldn’t be ruled out of your catalyst library, as there are ways to scale your product when limited by catalyst availability.  

In fact, Sinocompound has now announced their capability to provide commercial quantities of QPhos to scientists across the globe. Aided by their new purpose-built facility in Tongling, China, access to kilo scale quantities of QPhos is now a reality – meaning you can be confident including it in your screening library.

Dr Carin Seechurn, Associate Director – Technology Solutions, Sinocompound, is excited by the possibilities now opened by this achievement. “Our capability to scale-up the QPhos ligand represents a significant milestone in improving ligand accessibility for researchers. As we continue to expand our manufacturing processes thanks to our new plant in Tongling, we’re excited to provide more overlooked ligands and products commercially,” she says.

Broadening horizons

It’s not just phosphine-based ligands such as QPhos that you can collaborate with specialists to obtain. Sinocompound can work with you on custom synthesis projects for development of other non-commercially available catalysts/ligands and niche catalyst derivatives – delivering your required catalysts and ligands from gram to kilo scale in just 16 weeks.

Thanks to Sinocompound’s in-house team of ligand and metal catalyst experts, you don’t have to let non-commercial availability get in the way of your process development. And, you don’t have to let lack of a suitable catalyst hinder your project either. Sinocompound also offers catalyst screening services in partnership with InCatT, to help find you the right catalyst for your project and produce it in the quantities you need.

If you’re interested in how Sinocompound’s products and services – including catalyst screening and custom synthesis solutions – can speed-up your route to market, read more on our website: https://en.sinocompound.com/Products_Services.html

1. N. Kataoka, Q. Shelby, J. P. Stambuli, J. F. Hartwig, J. Org. Chem. 2002, 67, 16, 5553–5566.

2. a) N.A. Beare, J.F. Hartwig, J. Org. Chem, 2002, 67, 541-555; b) T. Hama, D.A. Culkin, J.F. Hartwig, J. Am. Chem. Soc. 2006, 128, 4976-4985; c) T. Hama, J.F. Hartwig, Org. Lett. 2008, 10, 1549-1552.

3. Ohtake, T. Sato, T. Kobayashi, M. Nishimoto, N. Taka, K. Takano, K. Yamamoto, M. Ohmori, M. Yamaguchi, K. Takami, S.-Y. Yeu, H.-H. Ahn, H. Matsuoka, K. Morikawa, M. Suzuki, H. Hagita, K. Ozawa, K. Yamaguchi, M. Kato, S. Ikeda, J. Med. Chem. 2012, 55, 7828-7840.

4. X. Dai, Y. Chen, S. Garrell, H. Liu, L.-K. Zhang, A. Palani, G. Hughes, R. Nargund, J. Org. Chem. 2013, 78, 7758-7763.