Boronic acids and boronate esters are commonly used reagents in Suzuki–Miyaura coupling chemistry. Organoboron derivatives are common reagents for C–C bond formation, either through classical palladium-mediated transformations or through other newer coupling methods. Boronic esters and acids are potential intermediates in the manufacture of many active pharmaceutical ingredients (API).
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Recently, Nuvation Bio announced positive pooled data from the pivotal Phase 2 TRUST-I and TRUST-II studies at the European Society for Medical Oncology (ESMO). Analysis showed that its small molecule taletrectinib, a new highly selective ROS1/NTRK kinase inhibitor, can cross the patient's blood-brain barrier to treat brain metastases, and nearly 90% of patients with advanced ROS1-positive non-small cell lung cancer (NSCLC) who received treatment had tumor shrinkage. In patients who had never been treated with tyrosine kinase inhibitors (TKIs), disease remission was sustained for nearly 4 years. Nuvation Bio plans to submit a new drug application (NDA) for the drug to the FDA in the fourth quarter of this year. Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.
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