From coal to cures: Chinese scientists bring a 160-year-old dream to life

Chinese scientists have discovered a way to turn cheap coal into valuable ingredients for medicine. This was once a long and difficult process, but now they have found a surprising short cut. In a study published on March 16 in the journal Nature, Jiao Ning’s team at Peking University solved a chemical puzzle that had confounded scientists for over 160 years. They successfully transformed inexpensive and readily available industrial feedstock – olefins – into high-value alkynes under mild and efficient conditions. This breakthrough not only revolutionises the concepts of molecular synthesis but also opens a gateway for China’s coal-based chemical industry to venture into the production of high-value-added fine chemicals. This exemplifies the strategic thinking that has guided China’s chemical industry in recent years: without needing more oil, China’s chemical industry can improve and create more value through new ideas. To grasp the significance of this achievement, one must first understand two fundamental building blocks of organic chemistry: olefins and alkynes. Olefins are compounds containing a carbon-carbon double bond. This bond, structurally akin to a “bent line”, is relatively reactive. Globally, olefins such as ethylene and propylene are produced on a large scale and at low cost, often by heating oil. In China, they are also made from coal, using a process that turns coal into methanol and then into olefins. This is especially important for China because the country has plenty of coal but very little oil. Alkynes, on the other hand, feature a carbon-carbon triple bond. This triple bond creates a linear structure with unique reactivity and geometry, making it a crucial module for constructing complex drugs such as the antibacterial retapamulin, the antiviral grazoprevir and the anticancer drug erlotinib, as well as common herbicides and insecticides. In essence, olefins are abundant and cheap, while naturally occurring alkynes are scarce. Alkynes are primarily obtained through complex chemical synthesis, resulting in limited yields and high costs, while drug and materials companies need them badly. So, turning inexpensive olefins into valuable alkynes would undoubtedly yield immense economic benefits. The idea of turning olefins into alkynes first appeared in 1861. However, traditional methods required extreme conditions such as high temperatures and strong bases – akin to cracking a nut with a sledgehammer. These harsh conditions were not only inefficient but also destroyed other sensitive “fine structures” within the molecule, severely limiting their practical application. For over 160 years, this remained an unresolved challenge. Rather than making minor improvements to the old methods, Jiao’s team charted a new course by reviving a long-forgotten special reagent: selenanthrene. The chemical was first made in 1896 but had been ignored for over 130 years. No one had ever used it in any synthetic reaction. After years of study, the team found it had a special ability: it could easily attach to an olefin, change its structure and then detach without leaving anything behind. The team created a new method that brought this old chemical back to use. The process works like careful surgery at the molecular level. First, the chemical attaches to the olefin’s double bond. Then, under gentle conditions, it reshapes the molecule, turning the bent bond into a straight one. After finishing this change, the chemical can be removed from the target molecule and recovered for reuse. This technology is not only mild but also highly efficient and practical. It can also separate different forms of the same molecule. This control over a molecule’s 3D shape helps scientists make drugs that work the right way. The scientific achievement solves a problem that stumped chemists for 160 years. But for China, the industrial impact is even more important. This research provides the key technology to truly turn coal into gold. China already had a way to turn coal into olefins. This helped reduce the country’s need for imported oil. But those olefins were mostly used to make cheap plastics. Jiao’s breakthrough creates a new path forward. These same coal-based materials can be used to make high-value chemicals, especially ingredients for new medicines. This means coal can now be used to produce key parts of cancer and antiviral drugs that are worth much more. Yet the journey from laboratory discovery to industrial application takes time. An expert based in Beijing, who spoke on condition of anonymity, suggested that when scaling up this technology for large-scale industrial production, challenges such as the scale-up effect might arise and would need to be further tested in practice.

From coal to cures: Chinese scientists bring a 160-year-old dream to life

.css-1c6uqr6{color:inherit;font-weight:inherit;font-size:inherit;font-family:inherit;line-height:inherit;overflow-wrap:break-word;}Study cracks a puzzle that has baffled scientists and may reshape modern medicine production as the world reels from a global oil shortage

Study cracks a puzzle that has baffled scientists and may reshape modern medicine production as the world reels from a global oil shortage