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微波条件下强固体酸催化快速高效合成外消旋巴洛沙韦
Crystals ( IF 2.4 ) Pub Date : 2022-06-23 , DOI: 10.3390/cryst12070891 Yiyun Wang , Xiaofang Lv , Zihui Meng , Zhibin Xu , Zhonghui Zheng , Jiarong Li , Min Xue
Crystals ( IF 2.4 ) Pub Date : 2022-06-23 , DOI: 10.3390/cryst12070891 Yiyun Wang , Xiaofang Lv , Zihui Meng , Zhibin Xu , Zhonghui Zheng , Jiarong Li , Min Xue
化合物 (±)-12aR-12-[(11S)-7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl]-7-hydroxy-3,4,12,12a- tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione是baloxavir marboxil的中间体。文献中采用传统的加热方法和普通的酸催化剂,反应时间长,收率低。因此,寻找一条高效、环保的合成路线势在必行。在这项研究中,(±)-12aR-12-[(11S)-7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl]-7-benzyloxy-3,4,12,使用磺酸盐合成 12a-四氢-1h-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione(化合物 3)微波条件下的树脂固体酸催化剂(HND-580)。不经进一步纯化除去苄基,得到中间体,外消旋巴洛沙韦,在微波照射下获得。两步总收率为78%。这种方法大大缩短了反应时间,提高了生产效率。
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更新日期:2022-06-23
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