In 2000, the FDA approved 26 new drug entities. This survey groups these therapeutics into four areas coded: (A) neurotransmitter analogs, (B) anti-ulcer and antiinflammation agents, (C) hormone-related drugs, and (D) antiinfectious drugs and miscellaneous molecules. Included in the synopsis for each compound is a description of the drug's benefits for a medical need, a mode of action if known, a chemical structure, and in most cases an abbreviated pathway outlining how the drug is synthesized.

The Schiff base derived from the condensation of o-aminophenol with benzaldehydes was induced to undergo oxidative cyclization in the presence of DDQ. The resulting 2-arylbenzoxazoles were separated from the reduced DDQ byproduct by treatment of reaction mixture with a strongly basic ion-exchange resin. The applicability of this chemistry to spatially separate library synthesis is demonstrated by the preparation of a 352-member library.

A series of novel 2'-fluoro-3'-[alkyl(hydroxy)amino]nucleoside analogs were prepared via conjugate addition of N-methylhydroxylamine to various 2-fluorobutenolides. The conjugate adducts 13a and 16 were obtained as single isomers under absolute control of stereochemistry. The crucial N-demethylation of the N-methylhydroxylamines 23-25 was readily achieved by means of DDQ oxidation, followed by nitrone/oxime exchange reaction. By this procedure, a variety of alkyl groups could be efficiently introduced at the 3'-N-atom of the nucleoside analogs, some of which might display potentially interesting anti-HIV properties.

“动态组合化学”（Dynamic Combinatorial Chemistry）利用分子自我组装的新方法形成“动态组合库”（Dynamic Combinatorial Library）。与传统组合化学技术相比，动态组合化学增加了“靶标模板”（Target Template）方法，模板的加入诱导了组合库内的分子组分的持续可逆的化学转化，产生新的组合库。该库的成份具有与模板相互作用的功能，有的成份是模板的最佳结合伙伴。如果建立的模板是为了筛选药物，这一技术可以应用于先导化合物（Lead Compounds）的发现过程。

在抗病毒研究过程中，核苷类型的RT抑制剂扮演着重要的角色。从经典的AZT到L-型核苷及至最近的磷酸前药，人们一直都在核苷的结构上大做文章，并逐渐认识到了L-型核苷的重要性。为了得到疗效更强，毒性更低的抗HIV、HBV的药，新的发展方向是对已有疗效比较好的化合物进行单磷酸化，使之能够在细胞内快速的变成三磷酸。随之需要解决的新问题，就是如何把磷酸盐变成中性的前药，以便进入细胞，然后在细胞内再变为有活性的磷酸盐。本综述讨论了几个L-核苷类似物的研究工作，对它们的合成、磷酸前药的研制方法、抗癌症的生物活性进行描述。