Background and overview[1]
Phenylboronic acid is a white solid. The melting point is 215~216℃ (anhydride), Ka13.7, and the dissolution state at 25℃ is: 1.75% (benzene), 1.2% (xylene), 30.2% (diethyl ether), 178% (methanol), 2.5% (water). It will automatically transform into phenylboron oxide C6H5BO in dry air. This transformation can also be completed by removing water by constant boiling with toluene. It is prepared by the reaction of phenyl magnesium bromide with methyl borate and can be used in organic synthesis.
2-Cyano-6-methoxyphenylboronic acid neopentyl glycol ester is a phenylboronic acid derivative, which can be used as a pharmaceutical synthesis intermediate and an organic synthesis intermediate. It is mainly used in laboratory research and development processes and chemical medicine. During the synthesis process. If neopentyl glycol 2-cyano-6-methoxyphenylborate is inhaled, move the patient to fresh air; if skin contact occurs, remove contaminated clothing and wash skin thoroughly with soap and water, e.g. If you feel unwell, seek medical attention; if contact with eyes occurs, separate eyelids, rinse with running water or methoxybutanol saline, and seek medical attention immediately; if ingested, rinse mouth immediately, do not induce vomiting, and seek medical attention immediately.
Preparation[1]
2-Cyano-6-methoxyphenylboronic acid neopentyl glycol ester can be used as a pharmaceutical synthesis intermediate. For example, N-(5-chloro-7-aryl-2,6-naphthyridin-3-yl)cyclopropanecarboxamide (1 equivalent), 2-cyano-6-methoxyphenylboronic acid neopentyl free di Silica glycol ester (2 equiv), bis(di-tert-butyl(4-dimethylaminophenyl)phosphine)palladium(II) dichloride (0.1 equiv) and 2.0 M sodium carbonate in water (4 equiv ) in acetonitrile under microwave irradiation (CEM microwave, 200 Watts) between 100°C and 150°C until the reaction is considered complete. The reaction mixture is then cooled, diluted with water and extracted with a suitable solvent.
Main reference materials
[1] Dictionary of organic compounds
[2]CN201180060626.6-substituted 6,6-fused nitrogen-containing heterocyclic compounds and their uses. Hoffmann-LaRoche Co., Ltd.
