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A Concise and Efficient Synthesis of Dapagliflozin
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2019-06-27 00:00:00 , DOI: 10.1021/acs.oprd.9b00141
Jun Yu 1 , Ying Cao 1 , HaiZhou Yu 1 , JinJia Wang 1
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2019-06-27 00:00:00 , DOI: 10.1021/acs.oprd.9b00141
Jun Yu 1 , Ying Cao 1 , HaiZhou Yu 1 , JinJia Wang 1
Affiliation
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A concise and efficient synthesis of the SGLT-2 inhibitor dapagliflozin (1) has been developed. This route involves ethyl C-aryl glycoside 9 as the key intermediate, which is easily crystallized and purified as the crystalline n-propanol solvate with high purity (>98.5%). The tetra-O-unprotected compound 9 could be directly reduced to crude dapagliflozin with high diastereoselectivity. The final pure API product 1 was isolated and purified with high purity (>99.7%). The process has been implemented on a multikilogram scale.
中文翻译:
Dapagliflozin的简便高效合成
已经开发了简洁高效的SGLT-2抑制剂dapagliflozin(1)的合成方法。该途径涉及作为主要中间体的乙基C-芳基糖苷9,其易于结晶和纯化为高纯度(> 98.5%)的结晶正丙醇溶剂化物。四-O-未保护的化合物9可以高非对映选择性地直接还原为粗制的达格列净。分离出最终的纯API产物1,并以高纯度(> 99.7%)进行纯化。该过程已在多千克规模上实施。
更新日期:2019-06-27
中文翻译:
![](https://scdn.x-mol.com/jcss/images/paperTranslation.png)
Dapagliflozin的简便高效合成
已经开发了简洁高效的SGLT-2抑制剂dapagliflozin(1)的合成方法。该途径涉及作为主要中间体的乙基C-芳基糖苷9,其易于结晶和纯化为高纯度(> 98.5%)的结晶正丙醇溶剂化物。四-O-未保护的化合物9可以高非对映选择性地直接还原为粗制的达格列净。分离出最终的纯API产物1,并以高纯度(> 99.7%)进行纯化。该过程已在多千克规模上实施。