The invention discloses a cyclovirobuxine D derivative and a preparation method and the application thereof. The structure of the derivative is shown as formula (I): R in the formula is selected from H, C1-6alkyl, phenyl, p-nitrophenyl, para halogen phenyl, para-C1-6alkyl substituted phenyl, para-C1-6alkoxy, para-trifluoromethyl-phenyl, para-dimethylamino-benzene base, inter-nitrophenyl, 3, 4-dimethyl-phenyl, 3, 4, 5- trimethyl-phenyl, 3, 4-dimethoxy-phenyl, 3, 4, 5-trimethoxybenzaldehyde base, 3-thiazolyl, 2-furyl or 1-naphthyl. The derivative can be prepared by taking cyclovirobuxine D and aldehydes (II) as raw materials. The derivative has the same effect as the cyclovirobuxine D, can be combined with pharmaceutically-acceptable auxiliary components into injection agent which can be used for treating cardiovascular and cerebrovascular disease and various oral pharmaceutical preparations.