Sonogashira偶联反应是构建碳碳三键、合成炔基类药物的核心工艺，在抗病毒药、抗真菌药、抗肿瘤靶向药等高端原料药生产中应用广泛。该反应采用钯-铜双金属协同催化，反应结束后体系中会残留钯、铜双重金属杂质，不仅要满足钯残留≤10ppm的药典要求，铜残留也需严格管控，加之炔基产物化学性质活泼，易氧化变质，对纯化材料的选择性、温和性提出了极高要求。
巯晟QSM112多齿巯基硅胶，凭借多齿配位基团的优势，可同步高效捕集钯、铜双金属离子，兼顾深度除杂与工艺温和性，完美适配Sonogashira偶联反应的纯化需求。产品不与炔基等活泼基团发生副反应，在四氢呋喃、乙腈、二氯甲烷等常用体系中，既能快速吸附金属残留，又能保护目标产物结构完整，杜绝产物氧化、变质，保障产品稳定性。
该产品吸附容量大、选择性强，可将钯残留降至0.3ppm以下，铜残留控制在1ppm以内，全面符合ICH及各国药典的金属残留限值。操作简便，无需复杂工艺调整，适配实验室小试到工业化大生产全流程，有效提升产品纯度与收率，降低纯化成本，解决双金属残留超标、产物易变质的行业难题，助力药企打造合规、高效、绿色的炔基药物合成工艺，推动高端原料药规模化生产与海外工艺转移。
Sonogashira coupling reaction is the core process for constructing carbon-carbon triple bonds and synthesizing alkynyl drugs, which is widely used in the production of high-end APIs such as antiviral drugs, antifungal drugs and antitumor targeted drugs. This reaction adopts palladium-copper bimetallic synergistic catalysis. After the reaction, dual metal impurities of palladium and copper will remain in the system. Not only the pharmacopoeia requirement of palladium residue ≤10ppm must be met, but also copper residue must be strictly controlled. In addition, alkynyl products are chemically active and easy to oxidize and deteriorate, which puts forward high requirements for the selectivity and mildness of purification materials.
Relying on the advantages of multi-tooth coordination groups, Qiusheng QSM112 Multi-tooth Mercapto Silica Gel can efficiently capture palladium and copper bimetallic ions simultaneously, taking into account deep impurity removal and process mildness, and perfectly adapting to the purification needs of Sonogashira coupling reaction. The product does not have side reactions with active groups such as alkynyl groups. In common systems such as tetrahydrofuran, acetonitrile and dichloromethane, it can not only quickly adsorb metal residues, but also protect the complete structure of the target product, prevent product oxidation and deterioration, and ensure product stability.
This product has large adsorption capacity and strong selectivity, which can reduce palladium residue to less than 0.3ppm and copper residue to less than 1ppm, fully meeting the metal residue limits of ICH and national pharmacopoeias. It is easy to operate, without complex process adjustment, adapting to the whole process from laboratory pilot test to industrial mass production, effectively improving product purity and yield, reducing purification costs, solving the industry problems of excessive bimetallic residues and easy deterioration of products, helping pharmaceutical enterprises create compliant, efficient and green alkynyl drug synthesis processes, and promoting large-scale production and overseas process transfer of high-end APIs.
