TSRI Chemists Devise Simple Method for Making Sought-After Boronic Acid-Based Drugs and Other Products Initial Demonstrations Yield Compounds with Promise for Treating COPD, Cystic Fibrosis and Other Lung Disorders
Co-authors of the study hold the ingredients to successfully carry out the new method. Left to right: David Peters, Ming Yan, Jie Wang, Chao Li and Lisa Barton. (Photo by Madeline McCurry-Schmidt.)
LA JOLLA, CA April 14, 2017 Chemists at The Scripps Research Institute (TSRI) have developed a broad and strikingly easy method for synthesizing a class of molecules that have demonstrated value as pharmaceuticals.
The difficulty of preparing these compounds boronic acids and closely related molecules known as boronate esters has greatly limited their use in the pharmaceutical industry, and to date there are only three FDA-approved drugs in this category.
With the new method, published this week as a First Release paper the journal Science, chemists can take abundant, inexpensive, structurally diverse compounds known as carboxylic acids and convert them easily into similarly structured boronic acids and related compounds.
Carboxylic acids are the ideal starting material for synthesizing boronic acids, but until now there hasn't been any method for getting from one to the other, said principal investigator Phil S. Baran, Darlene Shiley Professor of Chemistry at TSRI.
Among the boronic acid-derived molecules Baran and his team made in demonstrating the new method were several novel compounds that are now being investigated further as potential treatments for COPD and other lung disorders.
The development of the new method, known as decarboxylative borylation, follows a breakthrough made a year ago when Baran and his team were studying a reaction commonly used in laboratory chemistry as well as in nature: the amide-bond forming reaction, which among other things, helps stitch amino acids into proteins. We realized that the principles of amide bond formation, still the most utilized reaction in all of chemical synthesis, could be used to simplify a much broader set of molecule-building tasks, Baran said.
In this case, the insight enables the transformation of virtually any carboxylic acid, whether simple or complex, using just a single reaction step and inexpensive nickel catalysts. The new method essentially replaces a key carbon atom on a carboxylic acid with a boron atom.
Instead of devoting 95 percent of their effort to introducing a single boron atom, chemists can now easily install boron at any stage, Baran said.
Borylated versions of drug compounds should often have superior properties to their carboxylic acid counterparts. The new method for the first time makes it broadly practical for pharmaceutical chemists to create and investigate these borylated structures. To demonstrate, Baran and his team used the new method to make boronic acid versions of several common drugs, including Lipitor (atorvastatin) and vancomycin.
In a collaboration to demonstrate the translational utility of the discovery, Baran's team and chemists from the California Institute for Biomedical Research (Calibr), also used the method to make boronic acid-based compounds that inhibit a human enzyme known as neutrophil elastase. Immune cells release this enzyme within the lungs during infections and other conditions involving lung inflammation. Elastase is considered a major cause of the lung damage seen in COPD, cystic fibrosis, and related respiratory ailments.
To date, elastase inhibitors developed through other methods have shown limited effectiveness and/or significant side effects, and so far none has been FDA-approved. However, the team found in initial lab-dish tests that their boronic acid-based compounds inhibit elastase more strongly than older elastase-inhibiting compounds. We found that we could get a significant boost in potency by using a boronic acid group, said study co-author Arnab Chatterjee, director of medicinal chemistry at Calibr.
These boronic acid-based compounds can bind very tightly to their target molecules but in a way that allows them to detach eventually, thus potentially reducing the impact of off-target interactions that cause unwanted side effects.
The next step is to see how well these compounds perform in animal models, said Chatterjee. In general, this new method allows us in a practical way to get into this largely unexplored but promising chemical space of borylated compounds, and thus enables us to revisit old targets, such as elastase, that have largely resisted prior drug development efforts.
The co-lead authors of the paper, Decarboxylative borylation, were Chao Li and Jie Wang, postdoctoral research associates in the Baran Laboratory. Other co-authors were Lisa M. Barton, Maoqun Tian, David S. Peters, Anthony W. Yu and Ming Yan of TSRI; and Shan Yu, Manoj Kumar and Kristen A. Johnson of Calibr.
Funding was provided by the National Institutes of Health (grant GM-118176), Bristol-Myers Squibb, the China Scholarship Council, the Shanghai Institute of Organic Chemistry, Zhejiang Medicine Co., Pharmaron, Crohn's and Colitis Foundation of America and the German Research Foundation.
About The Scripps Research Institute
The Scripps Research Institute (TSRI) is one of the worlds largest independent, not-for-profit organizations focusing on research in the biomedical sciences. TSRI is internationally recognized for its contributions to science and health, including its role in laying the foundation for new treatments for cancer, rheumatoid arthritis, hemophilia, and other diseases. An institution that evolved from the Scripps Metabolic Clinic founded by philanthropist Ellen Browning Scripps in 1924, the institute now employs more than 2,500 people on its campuses in La Jolla, CA, and Jupiter, FL, where its renowned scientists includin
Most recent headlines
09/11/2025
Dalet today announced a transformative leap forward for media operations: Agentic Artificial Intelligence (AI) that unifies the Dalet ecosystem under one natura...
21/10/2025
As Amazon's Prime Video prepares to launch its coverage of NBA basketball under a major new deal, Grup Mediapro has announced that it is working with the st...
21/10/2025
ATLANTA Good news for consumers using an Atlanta DTH receiver to watch ATSC 3.0: with a new software update, they will be able to blanket their homes with Wi-Fi...
21/10/2025
While recent news has been heavily focused on Hispanic migration into the U.S., The 2025 Hispanic Market Report from Claritas highlights the fact that this gr...
21/10/2025
MAIDENHEAD, UK RWS has hired Michael Wayne as its head of media and entertainment in Los Angeles where he will lead the company's media localization busines...
21/10/2025
Imagine Communications and Rohde & Schwarz today announced a definitive agreement under which Imagine will acquire Pixel Power Limited, a wholly owned subsidiar...
21/10/2025
Atlanta DTH (ADTH) today announced a major update that will expand the functionality of its NEXTGEN TV receiver by enabling gateway capabilities allowing viewer...
21/10/2025
Heartland Video Systems, Inc. (HVS), a premier video systems integration, consulting, and expert ATSC 3.0 implementation firm announces that it has partnered wi...
21/10/2025
QuickLink, the leading provider of award-winning video production and remote guest integration solutions, today announced the appointment of Austin Hinton as it...
21/10/2025
nternet connectivity startup Miri Technologies Inc. will use this week's NAB Show New York as the launch pad for its latest ground-breaking innovation, the ...
20/10/2025
Inside TAMS: How Time-Addressable Media Stores could redefine sports workflows By Paul Markham
Friday, October 17, 2025 - 08:57
Print This Story
A penalty...
20/10/2025
Transformational production: Inside TVN's remote production push for the DFL...
20/10/2025
How NBC Sports Transitioned Stamford Facility to One Format: 1080p HDRMulti-year plan harmonizes workflows, simplifies operationsBy Ken Kerschbaumer, Editorial ...
20/10/2025
NBA on NBC' Studio Production Team Is Ready for Tip-Off With Coast-to-Coast...
20/10/2025
Under pressure: TVN CEO Markus Osthaus considers the German sports broadcasting ...
20/10/2025
(L-R) Maria Dizzia, Carmen Emmi, and Russell Tovey attend the Plainclothes pre...
20/10/2025
In March, we launched Concerts Near You to help listeners find concerts from their favorite artists. Since then, more than 3 million people have used it to disc...
20/10/2025
Em diversas cidades do Brasil, um movimento tem se fortalecido para celebrar o poder, a beleza e a profundidade da criatividade negra. O Dia AMPLIFIKA, agora em...
20/10/2025
In cities across Brazil, a movement is growing that celebrates the power, beauty, and depth of Black creativity. AMPLIFIKA Day, now in its fifth edition, return...
20/10/2025
Airborne Early Warning and Control aircraft rendering...
20/10/2025
DENVER and MUNICH Imagine Communications today announced its plans to acquire Pixel Power Ltd., a wholly owned subsidiary of Rohde & Schwarz. Financial terms of...
20/10/2025
LOS ANGELES G Morgan has joined Globecast, a provider of broadcast, media and entertainment managed services, as executive vice president of sales, Globecast Am...
20/10/2025
PLYMOUTH, Wisc. Heartland Video Systems and Zixi have partnered to enable broadcast-quality live video delivery over any IP network....
20/10/2025
A. R. Rahman on Facing Fear and Finding the Divine In an interview with Berklee President Jim Lucchese, the Oscar-winning composer reflects on how courage and...
20/10/2025
Monday 20 October 2025
To view this content, please enable our use of cookies. ...
20/10/2025
Rohde & Schwarz transfers Pixel Power to Imagine Communications Companies work collaboratively to ensure continuity and ongoing support for existing customers...
20/10/2025
RT 's Prime Time is set to host the final Presidential Election Debate this Tuesday night, October 21, providing an opportunity to hear directly from Irelan...
20/10/2025
NVIDIA and Google Cloud are expanding access to accelerated computing to transform the full spectrum of enterprise workloads, from visual computing to agentic a...
19/10/2025
Back to All News
Sins of Kujo' Comes to Life in New Live-Action Series Set for Spring 2026
Entertainment
19 October 2025
GlobalJapan
Link copied to cl...
18/10/2025
New England Sports Network (NESN) has chosen Harmonic, working with Astound Business Solutions, as its enterprise technology partner to transform primary distri...
18/10/2025
NEW ORLEANS, La. In the run-up to the start of the NBA season, WVUE-TV and Gray Local Media have announced a deal with DirecTV that will greatly expand access t...
18/10/2025
Berklee Celebrates 40 Years of the Fall Together Concert Faculty composers Bob Pilkington and Greg Hopkins are among the featured artists for this year's ...
17/10/2025
NEP Group Receives New Equity Investment From 26North Partners LP, Co-InvestorsCarlyle remains the largest shareholder as the company prepares for the futureBy ...
17/10/2025
Apple Lands Five-Year Deal for F1 Distribution in the U.S.Besides airing on Apple TV, the sport will be amplified on other Apple servicesBy Ken Kerschbaumer, Ed...
17/10/2025
SVG Sit-Down: Marshall Electronics' Bernie Keach on the Future of PTZ Camera...
17/10/2025
L2 Productions' REMI Facility in Austin Can Produce Content From AnywhereMusic festivals, sports events are produced via flypacks and remote control roomsBy...
17/10/2025
By Lucy Spicer
One of the most exciting things about the Sundance Film Festival...
17/10/2025
(L-R) Christopher Meyer, Addison Timlin, Cooper Raiff, Lili Reinhart, Alyah Chan...
17/10/2025
M sica e arte se uniram em uma noite especial na semana passada na ZIV Gallery, ...
17/10/2025
Music and art came together for one special night last week at ZIV Gallery, an i...
17/10/2025
Spotify and FC Barcelona are extending our partnership through 2030, continuing a collaboration that's redefining how fans, players, and artists connect. Th...
17/10/2025
MURRIETA, Calif. The Sports Fishing Championship (SFC) has deployed DigitalGlue's creative.space storage platform to streamline video production by centrali...
17/10/2025
BELLEVUE, Wash. Football continued to cement its reputation as a bulwark of TV advertising in Q3 2025 with new data from iSpot that showed both the NFL and coll...
17/10/2025
The Sports Fishing Championship (SFC), the premier competitive saltwater fishing series, has transformed its production workflow by adopting creative.space, the...
17/10/2025
QuickLink, a leading provider of award-winning multi-camera video productions and remote contribution solutions, announces the release of StudioPro Version 4, ...
17/10/2025
Although the annual Grammy Awards celebration is best known for recognizing achievements in the recording industry, the show often proves a visual spectacle as ...
17/10/2025
OpenDrives, Inc., a leading provider of software-defined data storage and data services, has promoted Alex Dunfey to Chief Technology Officer (CTO) from his for...
17/10/2025
The University of Arizona (UofA) has significantly upgraded its broadcast communication infrastructure with the integration of Riedel Communications' advanc...
17/10/2025
Harmonic (NASDAQ: HLIT) today announced that New England Sports Network (NESN), owned by Fenway Sports Group and Delaware North, has selected Harmonic as its en...
TSRI Chemists Devise Simple Method for Making Sought-After Boronic Acid-Based Drugs and Other Products Initial Demonstrations Yield Compounds with Promise for Treating COPD, Cystic Fibrosis and Other Lung Disorders
