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Ecofriendly Synthesis of Ribociclib Intermediate Using Regioselective Hydrodechlorination and DMAP Catalyzed Ester Hydrolysis
Topics in Catalysis ( IF 2.8 ) Pub Date : 2022-03-16 , DOI: 10.1007/s11244-022-01602-9 Allu Udayasri 1 , Manchikanti M. Chandrasekhar 1 , D. S. Ramakrishna 1 , P. Lakshmi Praveen 2 , M. V. N. Brahmeswararao 3 , Ganesh Varanasi 3
中文翻译：
区域选择性加氢脱氯和 DMAP 催化酯水解环保合成 Ribociclib 中间体
更新日期：2022-03-16
Topics in Catalysis ( IF 2.8 ) Pub Date : 2022-03-16 , DOI: 10.1007/s11244-022-01602-9 Allu Udayasri 1 , Manchikanti M. Chandrasekhar 1 , D. S. Ramakrishna 1 , P. Lakshmi Praveen 2 , M. V. N. Brahmeswararao 3 , Ganesh Varanasi 3
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This work reports the execution of Ecofriendly methods for the synthesis of Ribociclib precursor. Hazardous solvent free methodologies were optimized by using non hazardous and renewable solvents such as EtOH and DMSO. Highly abundant and biologically relavent Zinc metal was employed for Hydrodechlorination reaction along with Recommended solvent EtOH. DMAP catalyzed Ester hydrolysis reaction was performed using recommended solvent EtOH instead of MeOH. Amidation reaction was optimized using DMSO solvent instead of hazardous solvents such as DMF or NMP.
Graphical Abstract
中文翻译：
区域选择性加氢脱氯和 DMAP 催化酯水解环保合成 Ribociclib 中间体
这项工作报告了合成 Ribociclib 前体的环保方法的执行情况。通过使用无危险和可再生溶剂（如 EtOH 和 DMSO）优化无危险溶剂方法。高度丰富且生物相关的锌金属与推荐的溶剂 EtOH 一起用于加氢脱氯反应。使用推荐的溶剂 EtOH 代替 MeOH 进行 DMAP 催化的酯水解反应。使用 DMSO 溶剂代替 DMF 或 NMP 等危险溶剂优化酰胺化反应。
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