Chondroitin sulfate (CS) is one of the major and widespread glycosaminoglycans, a family of structurally complex, linear, anionic hetero-co-polysaccharides. CS plays a vital role in various normal physiological and pathological processes, thus, showing varieties of biological activities, such as anti-oxidation, anti-atherosclerosis, anti-thrombosis, and insignificant immunogenicity. However, the heterogeneity of the naturally occurring CS potentially leads to function unspecific and limits further structure-activity relationship studies. Therefore, the synthesis of CS with well-defined and uniform chain lengths is of major interest for the development of reliable drugs. In this review, we examine the remarkable progress that has been made in the chemical, enzymatic and chemoenzymatic synthesis of CS and its derivatives, providing a broad spectrum of options to access CS of well controlled chain lengths.

硫酸软骨素（CS）是一种主要且广泛使用的糖胺聚糖，是结构复杂，线性，阴离子杂共多糖的家族。CS在各种正常的生理和病理过程中起着至关重要的作用，因此显示出各种生物活性，例如抗氧化，抗动脉粥样硬化，抗血栓形成和微不足道的免疫原性。然而，天然存在的CS的异质性可能导致功能不确定，并限制了进一步的结构-活性关系研究。因此，具有确定的和均匀的链长的CS的合成对于开发可靠的药物具有重大意义。在这篇综述中，我们考察了CS及其衍生物的化学，酶促和化学酶促合成方面所取得的显着进展，