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Environmentally Benign and Facile Process for the Synthesis of Pantoprazole Sodium Sesquihydrate: Phase Transformation of Pantoprazole Sodium Heterosolvate to Pantoprazole Sodium Sesquihydrate
ACS Omega ( IF 4.1 ) Pub Date : 2017-09-06 00:00:00 , DOI: 10.1021/acsomega.7b00743
Arun Kumar Awasthi 1, 2 , Lalit Kumar 1 , Punit Tripathi 1 , Madhava Golla 1 , Mushtaq A. Aga 1 , Cirandur Suresh Reddy 2 , Pramod Kumar 1
Affiliation  

A cost-effective, scalable, and environmentally benign process is herein reported for the synthesis of pantoprazole sodium sesquihydrate: 5-(difluromethoxy)-2-[{(3,4-dimethoxy-2-pyridinyl)methyl}sulfinyl]-1H-benzimidazole sodium sesquihydrate. At least two of the three main synthetic steps (coupling and oxidation) have been carried out for the first time in water, with no need to isolate and purify the intermediates, affording the corresponding pantoprazole sodium in good yield and purity. Minimum organic solvents, in terms of both the number of solvents and the volume of solvent used, are employed to make this process both economical and environment friendly. Furthermore, in situ transformation of pantoprazole sodium heterosolvate, due to the association between molecules of water and solvent used, to pantoprazole sodium sesquihydrate is described.

中文翻译:

top托拉唑七水合物的合成的环境友好且简便的方法:Pan托拉唑异溶剂合物的相转化为Pan托拉唑七水合物

本文报道了一种经济高效,可扩展且对环境有益的方法,用于合成pan托拉唑倍半水合物:5-(二氟甲氧基)-2-[{((3,4-二甲氧基-2-吡啶基)甲基}亚磺酰基] -1 H-苯并咪唑钠倍半水合物。首次在水中进行了三个主要合成步骤(偶联和氧化)中的至少两个,无需分离和纯化中间体,从而以良好的收率和纯度提供了相应的pan托拉唑钠。就溶剂的数量和所用溶剂的量而言,最少的有机溶剂被用于使该方法既经济又环保。此外,描述了由于使用的水分子和溶剂之间的缔合,将pan托拉唑杂溶剂钠原位转化为pan托拉唑倍半水合物。
更新日期:2017-09-06
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