Related Products of 105942-08-3In 2019 ,《Manufacture of the PI3K β-Sparing Inhibitor Taselisib. Part 2: Development of a Highly Efficient and Regioselective Late-Stage Process》 was published in Organic Process Research & Development. The article was written by St-Jean, Frederic; Remarchuk, Travis; Angelaud, Remy; Carrera, Diane E.; Beaudry, Danial; Malhotra, Sushant; McClory, Andrew; Kumar, Archana; Ohlenbusch, Gerd; Schuster, Andreas M.; Gosselin, Francis. The article contains the following contents:
A highly efficient and regioselective manufacturing route for the phosphoinositide 3-kinase β-sparing inhibitor taselisib (I) was developed. Highlights of the synthesis include: (1) magnesium-mediated formation of a challenging cyclic amidine; (2) regioselective imidazole construction via alkylation/condensation with bromopyruvic acid; and (3) triazole formation with 2-iso-Pr acetamidrazone to generate the key bromobenzoxazepine core intermediate. Subsequent highly efficient one-pot palladium-catalyzed Miyaura borylation/Suzuki cross-coupling/saponification, followed by a 1,1′-carbonyldiimidazole-mediated coupling with ammonia, led to the pentacyclic taselisib. This new synthetic approach provides a more efficient route to taselisib with a significant decrease in process mass intensity compared to the previous early development routes to the bromobenzoxazepine core. Finally, implementation of a controlled crystallization provided the active pharmaceutical ingredient with the desired polymorphic form.4-Bromo-2-fluorobenzonitrile(cas: 105942-08-3Related Products of 105942-08-3) was used in this study.
4-Bromo-2-fluorobenzonitrile(cas:105942-08-3) is used as a OLED intermediate, Pharmaceutical, electronic and chemical intermediate.Related Products of 105942-08-3 It is used in the synthesis of heterocycles and liquid crystals.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts