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摘要：磷中心手性化合物的合成是过去三十年来逐渐发展起来的一个新兴领域。由于其作为配体在催化化学以及不对称有机合成中有重要应用、其广泛的生物活性使其在生物化学以及酶的抑制剂中有重要应用、作为原料药或者前药在医药领域有巨大的应用等等，使磷中心手性化合物的合成化学获得了迅猛发展。而作为一种磷手性化合物，H-亚磷酸酯及其衍生物在有机合成也有广泛在的应用。由于其自身具有廉价易得、易保存、化学反应活泼等优点，是合成a-胺基膦酸、环状a-羟基磷酸酯、双磷酸、核苷磷酸酯、环氧烷基磷酸酯、聚烯基磷酸酯等一系列重要化合物的原料。并且它还具有一定的杀菌灭菌作用，在医药农业领域也有相当广泛的应用。手性亚磷酸酯作为一种磷酰化基团能够和许多物质发生磷酰化反应，可以表现出多样的反应活性。正由于手性亚磷酸酯具有这些特点，所以手性亚磷酸酯在合成有机含磷功能化合物的应用是中外科学家的一个研究热点。通过查找大量资料表明，传统的手性亚磷酸酯类化合物的合成方法需在非常低的温度下才能反应。而随着手性亚磷酸酯类化合物的应用越来越广，不断增长的需求也对手性亚磷酸酯类化合物的合成方法有了新的要求，新的合成方法的研究也成了中外科学家的研究热点。本论文将以天然氨基酸作为手性源化合物，对在常温条件下合成手性亚磷酸酯类化合物进行初步探索。24724
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毕业论文关键词： 手性磷；亚磷酸酯；氨基酸
Design and Synthesis the phosphite compounds
Abstract: Synthesis of chiral compounds of phosphorus center is an gradually developed emerging field in the past three decades. Because of its important applications as ligands in asymmetric catalysis and organic synthesis chemistry . Its wide range of biological activity make it has important applications in biochemistry and enzyme inhibitors. As a raw material drug or prodrug in the field of medicine has great application, etc., so that the synthesis of chemical phosphorus center of chiral compounds gained rapid development. As one phosphorus chiral compound, H-phosphite and its derivatives are also widely used in organic synthesis applications. Because of its own with a cheap and easy to get, easy to preserve, lively chemical reactions, etc，it is a-amino acid synthesis, cyclic phosphate, diphosphate, nucleoside phosphates, epoxy alkyl esters, polyalkylene phosphate and a series of important raw materials. And it not only has a certain sterilization sterilization in the pharmaceutical field but also has a wide range of applications in agriculture. Chiral phosphite as a phosphoryl group, and many substances capable of phosphorylating reaction, can exhibit a variety of reactive activity. Precisely because chiral phosphite with these characteristics, it is used in synthetic organic chiral phosphite compound is a phosphorus-containing functional hotspot which China and foreign scientists focus on. Through research large amounts of data showed that the synthesis of the traditional method of chiral phosphite compounds need to react at very low temperatures. Because of the growing demand，the synthetic methods of chiral phosphite compounds have some new requirements, and the study of new synthetic methods has become a hot research in the world . This paper will be a natural source of amino acids as chiral compounds, to explore a new synthetic method of chiral phosphite compounds at room temperature.
Key words: Chiral phosphorus； Phosphite； Amino Acid
目 录
1 绪论 1
1.1引言 1
1.2 磷元素简介 1
1.3 磷与生物化学 2
1.4 磷与药物化学 3
1.4.1 含磷有机化合物在医药领域的应用 4