本論文分為三個部分: 第一部分為含硼一級胺之合成條件的優化 (Scheme 1)。實驗的結果顯示,產率相近的情況下,我成功地減少了2天的反應時間。 Scheme 1.含硼一級胺化合物之合成 由於含硼異腈化合物為高價值得合成材料 (Fig. 1),因此,第二部分主要是利用含硼一級胺為起始物,合成出含硼異腈化合物 (Scheme 2)。並利用此化合物作為起始物,合成出其相關的含硼衍生物。 Fig. 1. 含硼異腈在有機合成上之應用 Scheme 2. 含硼異腈化合物之合成 由於許多的藥物含有雜環的結構,因此,論文的第三部分為探討利用含硼異腈化合物來合成出一系列含硼雜環的化合物 (Scheme 3)。所得到的產率為86%-97% Scheme 3. 含硼四唑化合物之合成
This study is divided into three parts: First part, we have developed an optimal synthetic strategy (Scheme 1) to synthesize boron-containing amines (Scheme 1). The results of the experiment showed thatthe reaction time was reduced by 2 days when the yield was constant. Scheme 1. Synthetic condition of boron-containing primary amines Since the boron-containing isocyanides are high-value synthetic materials (Fig. 1), the second part uses boron-containing primary amines as the starting material to synthesize the boron-containing isocyanides (Scheme 2). We use the boron-containing isocyanides as starting materials to synthesize their related boron-containing derivatives. Fig. 1. Potential of boron-containing isocyanides in organic synthesis Scheme 2. Synthetic condition of boron-containing isocyanides Since many drugs contain heterocyclic structures, the third part is to explore the use of boron-containing isocyanides compounds to synthesize boron-containing tetrazoles (Scheme 3). The result of yields are86% -97%. Scheme 3. Synthetic condition of boron-containing tetrazoles