公开(公告)号：US20210009544A1

公开(公告)日：2021-01-14

申请号：US16975894

申请日：2018-07-30

申请人： Jiangsu Ruike Medical Science And Technology Co., Ltd.

发明人： Zhaobo Gao ,  Jianhua Chen ,  Zhidong Wan ,  Dawei He ,  Zengle Zhou ,  Xiaodong Ma ,  Wei Xiang ,  Jingxin Lin ,  Yijiang Mei

IPC分类号： C07D307/33 ,  C07D493/04 ,  C12P17/16 ,  C12P17/04

摘要： The invention relates to the field of pharmaceutical synthesis, in particular to a preparation method of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol derivatives and their intermediates. The preparation method is carried out starting from compound Formula A1. In the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol derivatives, the chirality was constructed by enzymatic method, and the products were prepared with high optical purity. The preparation method can be used to produce the key intermediates of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol of darunavir commercially, which is a very economical route suitable for industrial production.

公开(公告)号：US11535601B2

公开(公告)日：2022-12-27

申请号：US16975894

申请日：2018-07-30

申请人： Jiangsu Ruike Medical Science And Technology Co., Ltd.

发明人： Zhaobo Gao ,  Jianhua Chen ,  Zhidong Wan ,  Dawei He ,  Zengle Zhou ,  Xiaodong Ma ,  Wei Xiang ,  Jingxin Lin ,  Yijiang Mei

IPC分类号： C07D307/33 ,  C07D493/04 ,  C12P17/04 ,  C12P17/16

摘要： The invention relates to the field of pharmaceutical synthesis, in particular to a preparation method of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol derivatives and their intermediates. The preparation method is carried out starting from compound Formula A1. In the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol derivatives, the chirality was constructed by enzymatic method, and the products were prepared with high optical purity. The preparation method can be used to produce the key intermediates of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol of darunavir commercially, which is a very economical route suitable for industrial production.