The invention discloses a 
cytarabine analogue and a preparation method and application thereof. The 
cytarabine structural analogues P1-P4 are synthesized for the first time and can inhibit proliferation of 
leukemia cells HL60, and particularly, compared with Ara-C, the 
cytarabine structural analogues P4 are higher in 
leukemia cell proliferation inhibition capacity and 
cell penetration capacity, the concentration of the 
drug entering the cells and the concentration of the 
active metabolite cytarabine triphosphate generated in the cells are higher, and the 
bioavailability is higher; the cytosinearabinoside can be converted into a parent 
drug cytosine arabinoside in cells, so that the 
blood concentration of target cells 
in vivo is remarkably improved, and toxic and side effects and 
drug resistance caused by large-
dose medication can be avoided; and the half-life period of cytarabine is remarkably prolonged, the effective 
blood concentration is maintained for a long time, 
oral administration can be achieved, and inconvenience caused by injection medication can be avoided. The preparation method is simple, easy to operate and suitable for industrial production.