From lab to launch
BASF`s conference promoted the advantages of boron in synthetic chemistry

The second international BASF Boron Conference held recently in Tokyo met with an enthusiastic response. Around 100 international scientists and experts followed BASF’s invitation to exchange news and views about the latest developments in the field of boron chemistry.

The boron conference offers a platform for open discussions and scientific exchange as a way to establish contacts between scientists from institutes and industry, and especially our customers,” said Dr. Ulrich Bueschges, Group Vice President Inorganic Specialties at BASF in Ludwigshafen/Germany. “In this way we aim to further promote the industrial use of boron chemistry.”

From lab to launch: discover new horizons was the motto of the two-day conference, which was attended by scientists from academia and institutes, industrial R&D, and BASF customers. In total, 56 companies from eight countries were represented. The conference focused on the use of boron reagents in active ingredient synthesis, cross-coupling reactions, stereo- and regioselective reactions with boranes, and new applications for borane chemistry.
“No other conference so successfully brings together academic scientists and experts from industry working in the boron chemistry field,” said Professor Akira Suzuki of Hokkaido University, Japan.
“60 years ago, there were only two laboratories in the world capable of producing small amounts of diborane. Today, some of the best-selling medications are produced with the aid of organoboranes,” explained Dr. Carsten Blettner, Business Development Manager East Asia at BASF’s regional headquarters in Hong Kong.
The plenary lectures were given by the joint creators of the Suzuki-Miyaura coupling, Professor Akira Suzuki and Professor Norio Miyaura of Hokkaido University, Japan. BASF now operates the world’s largest plant for Suzuki-Miyaura couplings to produce the new fungicide boscalid in Guaratinguetá, Brazil. Professor Miyaura emphasized further reactions with boric acids during his presentation.
Amine-borane complexes, which can be used to perform particularly selective reductions, were discussed in detail by Professor Yasuo Kikugawa of Josai University, Japan: “Amine boranes are easy to handle, relatively nontoxic and have high stability,” he noted. The chemical reactivity of the reducing agent can be adjusted to match exactly the structure of the target molecule because of the large number of available amine-borane complexes. Kikugawa placed special emphasis on the advantages of picoline-borane, which BASF produces in commercial quantities.
In one of the decisive steps of the synthesis of coenzyme Q10 developed by Professor Sangho Koo, Myong Ji University, Korea, boron reagent LiBHEt3 (Calselect LT) has proved the most successful. Developed in the late 1990s as a laboratory synthesis, this process is now used successfully on a commercial scale and is constantly being refined.
The use of boron chemistry in pharmaceutical chemistry over the last 35 years were described by Dr. Om Reddy, Orchid Chemicals, India. “Boron reagents are excellent auxiliaries for process development,” said Dr. Karl Matos, BASF Corporation, Evans City, Pennsylvania. “They allow the synthesis of complex molecular structures with high selectivities and excellent yields.” This assessment was supported by Dr. Keshav Deo, Ranbaxy Research Laboratories, India.
The increasing commercial use of palladium-catalyzed borylation with pinacol boranes, such as PinB and Pin2B2 offered by BASF, was highlighted by Dr. Miki Murata, Kitami Institute of Technology, and Dr. Mayumi Nishida, Koei Chemical Company, Japan, and in a discussion of improved reagent systems by Akihiko Kojima. Palladium-catalyzed borylation with pinacol boranes is an addition to the Suzuki-Miyaura reaction and often makes it possible to reduce the number of process steps and achieve better results compared to conventional methods.
BASF is the market leader in the development and production of boron reagents for commercial organic synthesis. The company works closely with its customers to develop improved methods of synthesis for complex new molecules. Typical applications of boron reagents are the synthesis of active ingredients, OLED displays, and specialty chemicals. BASF’s portfolio includes highly selective boron reagents for reductions and hydroborylations, catalysts for asymmetric synthesis, and reagents for Suzuki couplings.
BASF produces boron specialties in Evans City, Pennsylvania/USA. The site’s wide array of experimental and production facilities allows the company to increase the production of reagents rapidly in response to demand, from process development to market launch.