N-(tert-Butoxycarbonyl)-D-prolinol → HCID 67019236, compound

Participants

Reaction Steps

Using an analogous procedure to that described for the preparation of the starting material in Example 11, tert-butyl (2R)-2-(hydroxymethyl)pyrrolidine-1-carboxylate (1.48 g, 7.37 mmol) was reacted with 4-(4-fluoro-2-methylindol-5-yloxy)-7-hydroxy-6-methoxyquinazoline (1.0 g, 2.95 mmol), (prepared as described for the starting material in Example 7), and the product purified by column chromatography, eluting with methanol/methylene chloride (1/9) containing 0.1% triethylamine to give tert-butyl (2R)-2-[(4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxyquinazolin-7-yloxy)methyl]pyrrolidine 1-carboxylate (970 mg, 62%).

Provenance & Evidence