公开(公告)号：US20220228184A1

公开(公告)日：2022-07-21

申请号：US17257792

申请日：2019-07-02

申请人： Merck Sharp & Dohme Corp.

发明人： Mark A. Huffman ,  Anna Fryszkowska ,  Joshua N. Kolev ,  Paul N. Devine ,  Kevin R. Campos ,  Matthew Truppo ,  Christopher C. Nawrat

IPC分类号： C12P19/40 ,  C12P17/04 ,  C12P9/00 ,  C12P7/18 ,  C07H13/00 ,  C07F9/113 ,  C07C33/042

摘要： The present invention relates to an enzymatic synthesis of 4′-ethynyl-2′-deoxy nucleosides and analogs thereof, for example EFdA, that eliminates the use of protecting groups on the intermediates, improves the stereoselectivity of glycosylation and reduces the number of process steps needed to make said compounds. It also relates to the novel intermediates employed in the process.

公开(公告)号：US12037623B2

公开(公告)日：2024-07-16

申请号：US17257792

申请日：2019-07-02

申请人： Merck Sharp & Dohme Corp.

发明人： Mark A. Huffman ,  Anna Fryszkowska ,  Joshua N. Kolev ,  Paul N. Devine ,  Kevin R. Campos ,  Matthew Truppo ,  Christopher C. Nawrat

IPC分类号： C12P19/40 ,  C07C33/042 ,  C07F9/113 ,  C07H13/00 ,  C12P7/18 ,  C12P9/00 ,  C12P17/04

CPC分类号： C12P19/40 ,  C07C33/042 ,  C07F9/113 ,  C07H13/00 ,  C12P7/18 ,  C12P9/00 ,  C12P17/04

摘要： The present invention relates to an enzymatic synthesis of 4′-ethynyl-2′-deoxy nucleosides and analogs thereof, for example EFdA, that eliminates the use of protecting groups on the intermediates, improves the stereoselectivity of glycosylation and reduces the number of process steps needed to make said compounds. It also relates to the novel intermediates employed in the process.