Pinanediol—a Key Intermediate for Boron-containing Drugs
Boron-containing drugs have achieved good therapeutic effects in anti-tumor, antibacterial, and other aspects. There are multiple boron-containing drugs on the market, such as lxazomib, Talabostat, Vaborbactam, etc.. But there are facing many challenges in the synthesis process, which are related to the instability and high activity of boric acid. Therefore, it is necessary to protect boric acid by introducing a protecting group during the synthesis process[1].
Pinanediol has unique advantages as a protecting group in the synthesis of boron-containing drugs[2]:
1. Commercial availability；
2. Mild reaction conditions and simple work-up;
3. Avoid the use of metal catalysts;
4. High yield and optical purity.
ChemExpress serves as your reliable global CRO & CDMO partner, we are capable of providing Pinanediol with mature technology, stable supply and production capacity of tons. Please contact us at 400-820-8665 or send email to [email protected]
Pinanediol
Application
Currently, Pinanediol has become one of the most popular boric acid protecting groups and it’s widely used in the synthesis of boron-containing drugs(Fig. 1). [3-5]
Fig. 1 Application of Pinanediol in the Synthesis of Boron-Containing Compounds
➤ We focus on providing RSMs, intermediates, APIs/HPAPIs, especially with high difficulty and high-performance process development, scale-up, and registration
➤ Products of raw materials and intermediate (100kg to tons) required for preclinical/clinical stage and commercialization
➤ Anti-tumor, anti-virus, diabetes, cardio cerebral Vascular disease treatment and other fields
➤ 120+ types of raw materials and intermediate products, of which 107+ products are commercialized
➤ Special Reactions: Grignard reaction, Oxidation reaction, Chlorination reaction, Hydrogenation reaction, High-pressure hydrogenation, Ultralow temperature reaction, Diazotization reaction, Nitration reaction, Chlorination reaction
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Reference:
[1] J. Chem. Soc., Perkin Trans. 1, 2002, 11, 1325-1339
[2] Molecules. 2020, 25, 4323.
[3] Future Med Chem. 2013, 5, 653-76.
[4] Acta Pharm Sin B. 2021, 11, 3035-3059.
[5] Pharmaceuticals (Basel). 2022, 15, 264.