Study On Preparation Technology Of Trifluoromethylpyridine Synthetic Block

Recently, it was discovered that when introduced into the molecular fluorine atom especially for trifluoromethyl, lipophilic compounds can be improved, thereby increasing the permeability of biological membranes and tissues, enhance the permeability of compounds. Thus, the introduction of a trifluoromethyl group in the molecule has become one of the commonly used methods for designing new drugs. So trifluoromethylpyridine Preparation of synthetic blocks of great practical significance.By Guizhou Wylton jinglin phosphorus Electronic Materials Co. Custom Synthesis 26 containing trifluoromethyl pyridine intermediates, which reported no routes have six(B3, B4, B5, C9, C10, C11), different from the literature the new synthetic route reported 5(A2, A4, D2, D3, D5), process optimization of existing routes there are 10(A1, B2, C3, C4, C5, C6, C12, D1, D2, D4).The optimum conditions for each step of the synthesis process were optimized by single factor experiment design, find the reactions: such as solvents, time, feed ratio, making the product yield have been greatly improved. The products of each step can be carried out structural characterization by mass spectrometry and NMR analysis methods, the results obtained are consistent with the product showed the desired product.