Heck偶联反应是实现烯烃官能化、构建复杂杂环药物的关键技术，在抗感染药、抗肿瘤药、心脑血管药物等原料药合成中不可或缺。该反应多在DMF、DMAc等高极性溶剂中进行，反应体系复杂，钯催化剂易与产物形成稳定络合物，常规除钯手段难以剥离，极易造成钯残留超标；同时传统除杂材料易出现溶胀、破损，不仅除钯效率低下，还会损耗产品收率，影响产物纯度，制约工业化生产效率。
巯晟QSM112多齿巯基硅胶，针对Heck偶联反应体系特性优化升级，多齿螯合基团能快速精准捕获溶解态、络合态钯金属，打破钯与产物的稳定结合，实现深度除钯。产品具备优异的高极性溶剂耐受性，在DMF、DMAc、乙腈等体系中依旧保持稳定结构，不溶胀、不破碎、无官能团溶出，杜绝二次污染，完美适配Heck偶联的工艺环境。
相较于传统除钯材料，QSM112吸附速率更快、处理周期更短，常温搅拌即可完成高效除钯，无需高温高压等严苛条件，简化生产流程。经药企实际应用验证，该产品可将Heck反应中间体钯残留从数百ppm降至0.5ppm以下，保证API产品纯度达标，有效减少收率损耗，提升溶剂回收效率，适配间歇式生产与连续化生产场景，助力药企优化纯化工艺，提升产品质量，满足高端原料药的生产与申报要求，打通医药合成工业化量产链路。
Heck coupling reaction is a key technology to realize olefin functionalization and construct complex heterocyclic drugs, which is indispensable in the synthesis of APIs such as anti-infective drugs, antitumor drugs and cardiovascular and cerebrovascular drugs. This reaction is mostly carried out in high-polarity solvents such as DMF and DMAc, the reaction system is complex, palladium catalyst is easy to form a stable complex with the product, conventional palladium removal methods are difficult to strip, and it is very easy to cause excessive palladium residue. At the same time, traditional impurity removal materials are prone to swelling and damage, which not only has low palladium removal efficiency, but also reduces product yield, affects product purity, and restricts industrial production efficiency.
Qiusheng QSM112 Multi-tooth Mercapto Silica Gel is optimized and upgraded according to the characteristics of Heck coupling reaction system. The multi-tooth chelating group can quickly and accurately capture dissolved and complexed palladium metals, break the stable combination of palladium and products, and realize deep palladium removal. The product has excellent high-polarity solvent tolerance, maintains a stable structure in DMF, DMAc, acetonitrile and other systems, no swelling, no breakage, no functional group dissolution, eliminates secondary pollution, and perfectly adapts to the process environment of Heck coupling.
Compared with traditional palladium removal materials, QSM112 has faster adsorption rate and shorter treatment cycle. It can complete efficient palladium removal by stirring at room temperature without harsh conditions such as high temperature and high pressure, simplifying the production process. Verified by practical application of pharmaceutical enterprises, this product can reduce the palladium residue of Heck reaction intermediates from hundreds of ppm to less than 0.5ppm, ensure the purity of API products, effectively reduce yield loss, improve solvent recovery efficiency, adapt to batch production and continuous production scenarios, help pharmaceutical enterprises optimize purification processes, improve product quality, meet the production and declaration requirements of high-end APIs, and open up the industrial mass production link of pharmaceutical synthesis.
