Substitution (Tosylate)

(N-Heteroaryls)

Examples:

Example 1

A mixture of the indole (A) (2.48 g, 10.0 mmol), the tosylate (B) (3.07 g, 12.0 mmol), and K2CO3 (4.14 g, 30.0 mmol) in DMF (40 mL) was stirred at 120 C overnight. The mixture was diluted with EtOAc (150 mL), washed with sat aq NaHCO3 (5 x 100 mL), dried (Na2SO4), and concentrated in vacuo to provide the product as a yellow oil. [3.3 g, 100%]

[Patent Reference: WO2016100281, page 201, (10.3 MB)]