Suzuki偶联反应是医药原料药、精细化工中间体合成中，构建碳碳键的核心工艺，尤其在沙坦类、抗肿瘤药、抗真菌药等联苯类药物生产中应用广泛。该反应依托钯催化剂完成催化偶联，但反应结束后，体系中残留的钯离子、钯黑难以彻底清除，极易出现钯残留超标问题，不仅难以满足ICH Q3D、各国药典严苛的金属残留限值要求，还会影响产品纯度、稳定性，甚至导致后续工艺副反应增多，成为药企规模化生产的共性痛点。
宁波巯晟新材料专为偶联反应除杂研发的**QSM112多齿巯基硅胶**，凭借多齿配位螯合技术，成为Suzuki偶联反应除钯的优选材料。相较于普通单齿巯基硅胶，QSM112采用高密度多齿巯基官能团键合工艺，对Pd(0)、Pd(II)均具备超强靶向吸附能力，吸附容量更大、选择性更高，可彻底摆脱传统活性炭吸附率低、离子交换树脂选择性差、溶剂兼容性弱的弊端。
该产品机械强度高，耐酸碱、抗溶胀，适配甲苯、乙醇、二氧六环、四氢呋喃等Suzuki偶联常用溶剂体系，常温常压下即可操作，无需改动原有生产工艺。实际应用中，可将原料药中间体钯残留从数百ppm稳定降至1ppm以下，远低于药典≤10ppm的标准，同时不破坏目标产物结构，不引入新杂质，保障产品HPLC纯度达标，提升工艺收率，还可再生重复使用，大幅降低药企纯化成本，助力药企顺利通过GMP核查、国际药典认证，适配医药中间体及原料药的工业化量产与工艺出海。
Suzuki coupling reaction is the core process for constructing carbon-carbon bonds in the synthesis of pharmaceutical APIs and fine chemical intermediates, especially widely used in the production of biphenyl drugs such as sartans, antitumor drugs and antifungal drugs. This reaction relies on palladium catalysts to complete catalytic coupling, but after the reaction, residual palladium ions and palladium black in the system are difficult to completely remove, which is very easy to cause excessive palladium residue. It not only fails to meet the strict metal residue limits of ICH Q3D and various national pharmacopoeias, but also affects product purity and stability, and even leads to more side reactions in subsequent processes, becoming a common pain point for large-scale pharmaceutical production.
**QSM112 Multi-tooth Mercapto Silica Gel** developed by Ningbo Qiusheng New Materials specially for impurity removal in coupling reactions has become the preferred material for palladium removal in Suzuki coupling reactions relying on multi-tooth coordination chelation technology. Compared with ordinary single-tooth mercapto silica gel, QSM112 adopts high-density multi-tooth mercapto functional group bonding process, which has super targeted adsorption capacity for both Pd(0) and Pd(II), with larger adsorption capacity and higher selectivity. It can completely get rid of the disadvantages of low adsorption rate of traditional activated carbon, poor selectivity of ion exchange resin and weak solvent compatibility.
This product has high mechanical strength, acid and alkali resistance, and swelling resistance. It is suitable for common solvent systems in Suzuki coupling such as toluene, ethanol, dioxane and tetrahydrofuran. It can be operated at normal temperature and pressure without changing the original production process. In practical application, it can stably reduce the palladium residue of API intermediates from hundreds of ppm to less than 1ppm, far lower than the pharmacopoeia standard of ≤10ppm. Meanwhile, it does not damage the structure of the target product, introduce new impurities, ensure the HPLC purity of the product, and improve the process yield. It can also be regenerated and reused, greatly reducing the purification cost of pharmaceutical enterprises, helping them smoothly pass GMP inspection and international pharmacopoeia certification, and adapting to industrial mass production and process overseas transfer of pharmaceutical intermediates and APIs.
