极具生理活性的含氮稠杂环及螺环化合物被广泛应用于各类抗癌及抗艾滋病药物中，而目前这类化合物的合成却存在反应条件苛刻、反应步骤长且无通用的合成方法的制约，因此破解这一难题便极具科研价值。结合我们多年的研究，本项目拟发展一种胺化反应方法学，来解决这一瓶颈问题。内容如下：（1）实施以Ti(NR1R2)4为氮源和诱导试剂的取代苯甲醛的胺化反应。给Ti(NR1R2)4的R基团中分别引入芳基、双键、三键、羰基等官能团，在室温下，不需贵金属催化剂，便可精准高效地合成分子中同时含有醛基、胺基、芳基（或双键、三键、羰基）三种官能团的苯甲醛，发展一种新的胺化反应方法学。（2）用得到的含有三种官能团的化合物为底物，实施吖啶、环氮二苯并[b,f][1,5]二氮芳辛和二苯二氮卓等20多类化合物的合成，发展一种通用的合成此类化合物的方法。（3）将发展的胺化反应方法学应用于一系列抗癌、抗艾滋病等药物的合成。

To overcome the lack of a general method for preparing nitrogen-containing fused heterocycles and nitrogen-containing spiro compounds, we will conduct the following researches. (1) Investigate the amination reactions of substituted benzaldehydes by using Ti(NR1R2)4 as both the nitrogen source and mediating reagent. By introducing an aryl (or a double bond, or a triple bond, or a carbonyl) group into the R group of Ti(NR1R2)4, we can synthesize a series of new benzaldehydes accurately and efficiently without using noble metal catalysts and phosphine ligands at room temperature. The synthesized benzaldehydes simultaneously bear an aryl- (or a double bond, or a triple bond, or a carbonyl), an aldehyde-, and an amine-group. Thus, a new efficient amination methodology will be developed. (2) Synthesize acridines, epiminodibenzo[b,f][1,5]diazocines and dibenzodiazepines by employing the compounds produced by the above-mentioned amination reactions and containing three functional groups, as the starting materials. Therefore a general method for preparing the nitrogen-containing fused heterocycles and nitrogen-containing spiro compounds is developed. (3) Apply the developed amination methodology to the synthesis of some important drugs, namely, the preparation of a series of anti-cancer, anti-AIDS and anti-Alzheimer drugs.