| 罗氟司特中间体3-环丙基甲氧基-4-二氟甲氧基苯甲醛的合成 |
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| 引用本文： | 周海洋,董旭,翟海民,陈明强. 罗氟司特中间体3-环丙基甲氧基-4-二氟甲氧基苯甲醛的合成[J]. 齐鲁药事, 2013, 0(11): 678-679 |
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| 作者姓名： | 周海洋 董旭 翟海民 陈明强 |
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| 作者单位： | 山东齐都药业有限公司,山东淄博255400 |
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| 摘 要： | 目的研究罗氟司特中间体的合成。方法 3,4-二羟基苯甲醛依次与Boc酸酐和氯甲基环丙烷反应后得3-环丙基甲氧基-4-O-Boc-苯甲醛,脱掉Boc后再与二氟一氯甲烷醚化制得罗氟司特中间体3-环丙基甲氧基-4-二氟甲氧基苯甲醛。结果总收率约62%。结论本合成路线操作简单,成本低,有利于大规模制备。
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| 关 键 词： | 3-环丙基甲氧基-4-二氟甲氧基苯甲醛 罗氟司特 中间体 合成 |
Synthesis of 3-cyclopropyl methoxy-4-difluoromethoxybenzaldehyde |
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| ZHOU Hai-yang,DONG Xu,ZHAI Hai-min,CHEN Ming-qiang. Synthesis of 3-cyclopropyl methoxy-4-difluoromethoxybenzaldehyde[J]. qilu pharmaceutical affairs, 2013, 0(11): 678-679 |
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| Authors: | ZHOU Hai-yang DONG Xu ZHAI Hai-min CHEN Ming-qiang |
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| Affiliation: | ( Shandong Qidu Pharmaceutical Co. , Ltd. , Zibo 255400, China ) |
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| Abstract: | Objective To study the synthesis of 3 - Cyclopropylmethoxy - 4 - difluoromethoxybenzaldehyde. Methods 3,4 - dihydroxybenzaldehyde via reaction with Boc anhydride and chloromethyl cyclopropane to obtain 3 - cyclopropyl methoxy -4 - O - Boc benzaldehyde, followed by deprotection and etherification with chlorodifluoromethane to synthesize the key intermediate of roflumilast. Results The overall yield was about 62%. Conclusion The synthetic route was simple, low cost and profit to lage - scale preparation. |
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| Keywords: | 3 - eyclopropyl methoxy - 4 - difluoromethoxybenzaldehyde Roflumilast Intermediate Synthesis |
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