The invention relates to benzocyclophosphamide phenate derivatives or pharmaceutically acceptable salts (I) thereof. The benzocyclophosphamide phenate derivatives or pharmaceutically acceptable salts thereof comprise stereoisomerides or tautomers. In the formula (I), R is 4-hydroxyphenyl, 4-methoxyphenyl, 4-acetoxy-phenyl, 3, 4-dihydroxyphenyl, 3, 4, 5-trihydroxyphenyl, 3, 4-dimethoxyphenyl, 3, 4, 5-trimethoxyphenyl, 3, 4-dihydroxy styryl, 3-methoxy-4-hydroxy styryl, 3, 4-dimethoxy styryl, 3, 4-diacetoxy styryl and 3-methoxy-4-acetoxy styryl. The benzocyclophosphamide phenate derivatives disclosed by the invention have significant anti-cancer effect, can effectively prolong the survival time of mice loaded with HL60, have better effects than the cyclophosphamide and have the obvious inhibitory action against the angiogenesis of a chorioallantoic membrane (CAM). Thus, the benzocyclophosphamide phenate derivatives disclosed by the invention can be applied to preparation of anti-tumor medicaments. The invention discloses the preparation method of the benzocyclophosphamide phenate derivatives.