(1-Benzothiophen-4-yl)boronic acid synthesis

Yield:177735-30-7 49%

Reaction Conditions:

with n-butyllithium;Triisopropyl borate in tetrahydrofuran at -78;

Steps:

14.1 Step 1. benzojbjthiophen-4-ylboronic acid (2-26)

A mixture of 4-bromobenzo[bjthiophene (2-25, 140 mg, 0.65 mmol), triisopropyl borate (122 mg, 0.65 mmol), and n-BuLi (0.52 mL, 0.65 mmol, 1.5M) in THF (5 mL) was stirred at -78 °C for 2 h. Upon reaction completion, the resulting mixture was washed with H20, extracted with ethyl acetate (50 mL x 3), concentrated under reduced pressure to provide intermediate 2-26 (yellow solid, 60 mg, 49% yield). LCMS (m/z): 177 [M + HI .

References:

WO2016/161145,2016,A1 Location in patent:Paragraph 00700