期刊论文

中文

合成化学

1005-1511

2024

32

5

393-399

10.15952/j.cnki.cjsc.1005-1511.23044

2022JJ80096:湖南省自然科学基金项目 YN22039:常州工学院基金资助项目

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在合成阿伐那非的经典路线中,最后一步反应使用了EDCI和HOBT作为酸胺缩合剂。HOBT中可能含有肼的残留,存在引入含酰肼结构的潜在致突变性杂质。通过化学方法合成阿伐那非潜在的基因毒性杂质E,即(S)-4-((3-氯-4...展开更多 在合成阿伐那非的经典路线中,最后一步反应使用了EDCI和HOBT作为酸胺缩合剂。HOBT中可能含有肼的残留,存在引入含酰肼结构的潜在致突变性杂质。通过化学方法合成阿伐那非潜在的基因毒性杂质E,即(S)-4-((3-氯-4-甲氧基苄基)氨基)-2-(2-(羟甲基)吡咯烷-1-基)嘧啶-5-羧酸(M6)与硫酸肼经酸胺缩合后得到(S)-4-((3-氯-4-甲氧基苄基)氨基)-2-(2-(羟甲基)吡咯烷-1-基)嘧啶-5-碳酰肼(杂...

In the classical route of the synthesis of avanafil, the last step of the reaction uses EDCI and HOBT as an acid and amine binding agent. HOBT may contain residues of hydrazine, and potential mutagenic impurities containing acylhydrazide structures may be formed. The po...MORE In the classical route of the synthesis of avanafil, the last step of the reaction uses EDCI and HOBT as an acid and amine binding agent. HOBT may contain residues of hydrazine, and potential mutagenic impurities containing acylhydrazide structures may be formed. The potentially genotoxic impurity E (Imp- E ) of avanafil...