tert-Butyl N-[1-(quinazolin-4-yl)piperidin-4-yl]carbamate synthesis

Yield:-

Reaction Conditions:

with N-ethyl-N,N-diisopropylamine in isopropyl alcohol; for 16 h;Heating / reflux;

Steps:

63.1

To a solution of 4-chloroquinazoline (2. 0 g, 12.2 mmol) in 45 mL IPA was added Boc-4-aminopiperidine (2.56 g, 12.8 mmol) and DIEA (3.2 mL, 18.2 mmol). The reaction mixture was heated to reflux and stirred 16 hours, after which the reaction mixture was cooled to room temperature and concentrated. The residue was dissolved in EtOAc and washed with water, 1N NaOH, brine, dried (Na2SO4), filtered, and concentrated to provide 4- (4-Boc- aminopiperidin-1-yl) quinazoline, which was used directly in the next step.

References:

WO2005/51304,2005,A2 Location in patent:Page/Page column 108