4-(2-hydrazinopyrimidin-4-yl)morpholine synthesis

Yield:-

Reaction Conditions:

with hydrazine in ethanol at 90; for 4 h;

Steps:

10.ii

To a solution of the appropriate 2-Chloro-pyrimidin-4-ylamine derivative (1 equiv, 46.1 mmol) in ethanol (45 ml) was added hydrazine hydrate (7.2 ml, 231 mmol). The mixture was heated to 90° C. under an inert atmosphere for 4 hours. The reaction was then cooled to 0° C. and the resultant precipitate collected by filtration. The collected product was washed with cold water and recrystallised from the minimum quantity of hot ethanol to give the desired product in suitably clean form to be used without further purification. 55a: NRR'=morpholino: m/z (LC-MSW, ESP):195.4 [M+H]⁺, R/T=0.37 mins.

References:

US2006/199804,2006,A1 Location in patent:Page/Page column 34