CAS: 184177-81-9; Phenyl (4-(4-(4-Hydroxyphenyl)Piperazin-1-yl)Phenyl)Carbamate

上下游产品

phenyl chloroformate 1-(4-aminophenyl)-4-(4-hydroxyphenyl)piperazine 4-amino-phenolacetic acid 4-[4-(4-phenoxycarbonylamino-phenyl)-piperazin-1-yl]-phenyl ester 2-[(1S,2S)-1-ethyl-2-benzyloxypropyl]-2,4-dihydro-4-[4-[4-(4-hydroxyphenyl)piperazin-1-yl]phenyl]-3H-1,2,4-triazol-3-one 4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-1-((2S,3S)-2-(benzyloxy)pentan-3-yl)-1H-1,2,4-triazol-5(4H)-one posaconazote

4-(4-(4-硝基苯基)-1-哌嗪基)苯酚置于氯化铵,锌体系中,用 四氢呋喃,甲醇 用作溶剂,化学反应 6.5H,反应生成[4-[4-(4-羟基苯基)-1-哌嗪基]苯基]氨基甲酸苯酯
参考文献:一种4-[4-[4-(4-羟基苯基)哌嗪-1-基]苯基]氨基甲酸苯酯的制备方法
标题:一种4-[4-[4-(4-羟基苯基)哌嗪-1-基]苯基]氨基甲酸苯酯的制备方法
摘要:本发明公开了一种4‑[4‑[4‑(4‑羟基苯基)哌嗪‑1‑基]苯基]氨基甲酸苯酯的制备方法,以4‑羟基苯胺为原料,先与二氯乙胺盐酸盐关环合成1‑(4‑羟苯基)哌嗪,纯度95A%,矫正收率80%;再由对硝基氯苯和制得的1‑(4‑羟苯基)哌嗪偶联合成4‑(4‑(4‑硝基苯基)‑1‑哌嗪基)苯酚,纯度93A%,矫正收率88%;然后硝基还原合成1‑(4‑氨基苯基)‑4‑(4‑羟基苯基)哌嗪,纯度98A%,矫正收率77%;最后由氯甲酸苯酯保护酚羟基合成4‑[4‑[4‑(4‑羟基苯基)哌嗪‑1‑基]苯基]氨基甲酸苯酯,纯度:98.7%,含量98.5Wt%,矫正收率83%.本发明能够通过易得的原料和简洁的工艺步骤获得高纯度的目标产物4‑[4‑[4‑(4‑羟基苯基)哌嗪‑1‑基]苯基]氨基甲酸苯酯.

专利信息

专利号:WO-2019077627-A1
优先权日:2017-10-16
标题:PROCESS FOR PRODUCING POSACONAZOLE
发明人：NANDEPU Venkateswara Rao; BIJJULA VENKATA KRISHNA REDDY; BATHINA Satyanarayana
权利人:METROCHEM API PVT LTD
摘要:The present invention relates to an improved process for the manufacture of Posaconazole, an antifungal agent belonging to the category of triazole compound substituted tetrahydrofuran. The present invention further relates to the preparation of Formula A and Formula B, key intermediates in the preparation of Posaconazole. The invention also relates to novel intermediates that are useful in the synthesis of Posaconazole.