α-Amino nitrile compounds have a profound impact on bio-chemical sciences, as they have been prepared from inexpensive starting materials and have become valuable intermediates in the chemical synthesis of vitally important heterocyclic and carbocyclic molecules, which serve as suitable models in pharmacological and biological research. The α-amino nitrile moiety has been found in the structure of different alkaloids, while the α-amidoacetonitrile group is an essential fragment of new anti-hyperglycemic drugs and promising pharmacological and agrochemical agents. Due to their synthetic, biological and practical importance, this review highlights the recent information about the preparation of α-amino nitriles through the Strecker-type and α-cyanation reactions, their chemical and biological properties, as well as their synthetic application, paying attention on the wonderful capacity for generating novel molecular diversity for pharmacological, biological and agrochemical researches, which ends with the total synthesis of complex alkaloids, preparation of new N-heterocycles and α-aminonitrile-containing drugs. Analyzing modern synthetic protocols for the Strecker-type reactions and cyanation reactions based on cross-dehydrogenative coupling (CDD) process, the advantages and disadvantages of new catalysts and green reaction conditions are also discussed. In addition, remarkable biological properties of α-amidoacetonitrile derivatives as potent and selective protease inhibitors as well as promising pesticidal agents were briefly reviewed. The bibliography includes 461 references.

α-氨基腈化合物是由廉价的起始原料制备的，已对生物化学产生了深远的影响，并已成为重要的杂环和碳环分子化学合成中的重要中间体，这些化合物可作为药理学和生物学领域的合适模型研究。已经在不同生物碱的结构中发现了α-氨基腈部分，而α-酰胺基乙腈基团是新的抗高血糖药物以及有希望的药理和农用化学试剂的重要片段。由于它们的合成，生物学和实用重要性，本综述重点介绍了有关通过Strecker型和α-氰化反应制备α-氨基腈的最新信息，其化学和生物学特性以及其合成应用，N-杂环和含α-氨基腈的药物。分析了基于交叉脱氢偶联（CDD）工艺的Strecker型反应和氰化反应的现代合成方案，并讨论了新型催化剂和绿色反应条件的优缺点。此外，简要回顾了α-酰胺基乙腈衍生物作为有效和选择性蛋白酶抑制剂以及有前途的杀虫剂的显着生物学特性。参考书目包含461个参考文献。