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Efficient Phosphorus-Free Chlorination of Hydroxy Aza-Arenes and Their Application in One-Pot Pharmaceutical Synthesis
Organic Process Research & Development ( IF 3.4 ) Pub Date : 2020-01-27 , DOI: 10.1021/acs.oprd.9b00407
Jian Wang 1, 2 , Yan-Hui Li 1 , Song-Cheng Pan 1 , Ming-Fang Li 1 , Wenting Du 2 , Hong Yin 2 , Jing-Hua Li 1
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The chlorination of hydroxy aza-arenes with bis(trichloromethyl) carbonate (BTC) and SOCl2 has been effectively performed by refluxing with 5 wt % 4-dimethylaminopyridine (DMAP) as a catalyst. Various substrates are chlorinated with high yields. The obtained chlorinated aza-arenes can be used directly with simple workup for succedent one-pot synthesis on a large scale.

中文翻译:

氮杂氮杂戊烯的高效无磷氯化反应及其在一锅法药物合成中的应用

用碳酸二(三氯甲基)酯(BTC)和SOCl 2氯化羟基氮杂芳烃已经通过与5重量%的4-二甲基氨基吡啶(DMAP)作为催化剂回流而有效地进行。各种底物都可以高产率氯化。所获得的氯化氮杂芳烃可通过简单的后处理直接直接用于大规模的一锅合成。
更新日期:2020-01-27
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