Peking University Breakthrough: Coal Derivatives to Medicines via Revolutionary Alkyne Synthesis

The Groundbreaking Discovery at Peking University

In a remarkable advancement for synthetic chemistry, researchers at Peking University have achieved a long-sought goal: transforming simple alkenes derived from coal into high-value alkynes essential for pharmaceutical production. This breakthrough, detailed in a March 16, 2026, publication in the prestigious journal Nature, addresses a chemical challenge first posed in 1861. Led by Professor Ning Jiao from the School of Pharmaceutical Sciences, the team developed a mild, efficient method using a recyclable selenanthrene reagent. This innovation not only streamlines the synthesis of complex drug molecules but also aligns with China's strategic push to leverage its vast coal reserves for high-tech applications.

Peking University, one of China's premier institutions, continues to lead in chemical innovation. The State Key Laboratory of Natural and Biomimetic Drugs, where Jiao's group is based, has a track record of pioneering green synthesis techniques. This discovery exemplifies how university research can bridge fundamental science with industrial needs, particularly in resource-rich sectors like coal chemistry.

The process begins with alkenes—olefins—produced via China's mature coal-to-olefins (CTO) technology. With over 36 CTO projects approved, boasting a combined capacity exceeding 24 million tonnes annually and investments surpassing 300 billion yuan, China dominates global olefin production from coal. Previously, converting these abundant alkenes to alkynes required harsh conditions, limiting scalability. Jiao's method changes that.

Historical Context: A 160-Year Puzzle

The quest to convert alkenes directly to alkynes dates back to 1861, when early chemists envisioned dehydrogenating the double bond (C=C) to form a triple bond (C≡C). Traditional approaches relied on elimination reactions using strong bases like sodium amide or high temperatures over 200°C, often destroying sensitive functional groups in drug precursors. Selenanthrene, synthesized in 1896, languished unused for over 130 years due to its overlooked potential.

This longstanding barrier hindered efficient production of terminal alkynes, which are pivotal in medicinal chemistry for click chemistry reactions, Sonogashira couplings, and constructing rigid molecular frameworks. Peking University's solution revives selenanthrene through a 'cascade activation' strategy, enabling room-temperature operation and broad substrate compatibility.

Professor Ning Jiao and the Innovative Team

Professor Ning Jiao, a distinguished figure in organic synthesis, heads the Jiao Group at Peking University. With expertise in C-H/C-C bond activation and entropy-driven processes, Jiao's lab focuses on sustainable routes to bioactive molecules. Named a Fellow of the Royal Society of Chemistry, he has published extensively on green methodologies.

The Nature paper lists co-first authors Junhong Meng, Yiqi Liang, and others, all from PKU's pharmaceutical and chemistry labs, with collaborators from Beijing University of Chemical Technology. This interdisciplinary effort underscores Peking University's strength in fostering collaborative research environments, attracting top talent through state key labs and funding like the National Natural Science Foundation of China.

Such teams exemplify the vibrant research culture at PKU, where young scientists gain hands-on experience in cutting-edge projects, preparing them for leadership roles in academia and industry.

The Chemistry Unveiled: Step-by-Step Mechanism

The method employs selenanthrene, which selectively binds to the alkene's double bond. Under mild conditions—typically room temperature with a photocatalyst or base—the reagent facilitates dehydrogenation, straightening the bond into an alkyne. Crucially, selenanthrene is regenerated post-reaction, achieving over 90% recyclability in lab tests.

1. Selenanthrene coordinates with the alkene π-system.
2. Cascade activation triggers hydrogen elimination.
3. Alkyne forms; reagent detaches and is recovered.

This contrasts sharply with prior methods' multi-step, low-yield processes. The paper demonstrates high yields (up to 95%) across 100+ substrates, including halides, esters, and heterocycles. Notably, it inverts or sorts Z/E isomers, enabling stereoselective drug synthesis—a feat impossible before.Read the full Nature study here.

Pharmaceutical Applications: From Lab to Lifesaving Drugs

Terminal alkynes are scaffolds in over 20 FDA-approved drugs. Examples include:

• Retapamulin: Topical antibacterial for skin infections.
• Grazoprevir: Antiviral for hepatitis C.
• Erlotinib: Anticancer agent targeting EGFR mutations in lung cancer.

Statistics show alkynes feature in 15-20% of new small-molecule drugs annually, per analyses from pharmaceutical databases. This PKU method cuts synthesis steps by 50-70%, reducing costs and waste. Late-stage functionalization allows direct modification of advanced intermediates, accelerating drug discovery pipelines at Chinese pharma giants like Hengrui and Innovent.

In higher education, such tools empower university labs to prototype drug candidates, fostering partnerships with industry.SCMP coverage highlights pharma potential.

Linking to China's Coal-to-Chemicals Revolution

China's coal-to-olefins (MTO) capacity hit 24+ million tonnes in 2026, with projects like Baotou's DMTO-III (1.35Mt/year olefins). Converting these cheap feedstocks to alkynes upgrades low-value coal products to fine chemicals, supporting 'dual carbon' goals by minimizing oil imports (China imports 70% of oil).

Peking University's work positions universities as innovation hubs for resource transformation, aligning with national strategies like the 14th Five-Year Plan emphasizing CTO upscaling.

Sustainability and Green Chemistry Advantages

The recyclable catalyst reduces waste by 80% versus traditional routes. Mild conditions preserve functional groups, enabling atom-economical synthesis. This entropy-driven process exemplifies green principles, vital for sustainable pharma amid global ESG pressures.

At PKU, such research trains students in eco-friendly methodologies, preparing them for green jobs in China's burgeoning chemical sector.

Challenges Ahead and Scaling Prospects

Lab success (gram-scale) must translate to industrial tons. Experts note potential scale-up issues like catalyst stability. PKU's ties to enterprises like Sinopec position it well for pilots.

Future: Optimize for continuous flow reactors; expand to polymer upcycling, per Jiao Group's polyolefin work.

Impact on Chinese Higher Education and Research Landscape

This Nature paper elevates PKU's global ranking (top 20 QS Chemistry 2026). It attracts funding, talent, and collaborations, boosting PhD/postdoc opportunities in organic synthesis.

China's universities produced 1.27M STEM grads in 2026; breakthroughs like this drive R&D investments, creating faculty positions in key labs.

Global Recognition and Expert Perspectives

PKU's Facebook and Twitter buzzed with shares, trending in chemistry circles. International chemists praise the 'elegant revival' of selenanthrene.

Anonymous Beijing expert: 'Practical for pharma; scaling key.' Aligns with global shifts to sustainable feedstocks.

Career Opportunities in Coal-Derived Chemistry at Chinese Universities

This breakthrough opens doors: postdocs in Jiao Group, faculty at PKU/Shenzhen campuses, industry roles at CTO firms. With /research-jobs booming, explore research positions or faculty openings in China.

Skills in catalysis, green synthesis highly sought; PKU grads average 150k RMB starting salary in pharma R&D.

Photo by Kelsey He on Unsplash

Future Outlook: Transforming Coal into a Pharma Powerhouse

As China eyes 30Mt CTO by 2030, PKU's method could spawn billion-yuan industries. Universities like PKU will lead, training next-gen chemists for dual-circulation economy. This isn't just chemistry—it's a blueprint for innovation-driven growth.