Reacción #85826

Ecuación de reacción

2-chloro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine

pyrrolidin-3-ol

DIPEA

→

desired compound

6-(3-hydroxypyrrolidin-1-yl)pyridin-3-ylboronic acid

Disolventes

NMP

Condiciones de reacción

Tratamiento posterior

1. 1
   Otrothe mixture was sealed in a microwave tube

Procedimiento

To a solution of 2-chloro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine (239 mg, 1 mmol) in NMP (2 mL) was added pyrrolidin-3-ol (174 mg, 2 mmol) and DIPEA (500 uL, 3 mmol), then the mixture was sealed in a microwave tube and heated in microwave reactor at 180° C. for 1.5 hours. TLC and LC-Ms showed the reaction had completed and the desired compound was detected. The reaction mixture was poured into 30 mL of H2O, and extracted with n-BuOH, washed with water and brine, concentrated and purified on TLC(CH2Cl2:MeOH=10:1) to give a white solid. MS (m/z): 209 (M+H)+

Fuente