Title:
ENZYMATIC SYNTHESIS OF 4'-ETHYNYL NUCLEOSIDE ANALOGS
Document Type and Number:
Japanese Patent JP2023123750
Kind Code:
A
Abstract:
To provide a synthesis method of 4'-ethynyl 2'-deoxy nucleosides and analogs thereof that eliminates the use of protecting groups on intermediates, improves the stereoselectivity of glycosylation, and reduces the number of process steps needed to make the compounds.SOLUTION: A method for synthesizing a 4'-ethynyl 2'-deoxy nucleoside or an analog thereof comprises combining compound 6.5 in the figure [where 2X+ is (a) two protons, (b) one proton and one monovalent cation, (c) two monovalent cations which are the same or different, or (d) one divalent cation] with purine nucleoside phosphorylase and a nucleobase or an analog thereof, in a buffered solution containing a manganese (II) salt.SELECTED DRAWING: None
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Inventors:
MARK A HUFFMAN
ANNA FRYSZKOWSKA
JOSHUA N KOLEV
PAUL N DEVINE
KEVIN R CAMPOS
MATTHEW TRUPPO
CHRISTOPHER C NAWRAT
ANNA FRYSZKOWSKA
JOSHUA N KOLEV
PAUL N DEVINE
KEVIN R CAMPOS
MATTHEW TRUPPO
CHRISTOPHER C NAWRAT
Application Number:
JP2023107449A
Publication Date:
September 05, 2023
Filing Date:
June 29, 2023
Export Citation:
Assignee:
MERCK SHARP & DOHME LLC
International Classes:
C12P19/40; A61K31/7076; A61P31/18; C07C29/74; C07C33/042; C07F9/655
Attorney, Agent or Firm:
Makoto Ono
Kennori Kanayama
Yoshiyuki Tsubokura
Kazuki Shigemori
Kenji Ando
Hidehiko Ichikawa
Yoshie Sakurada
Yosuke Kawasaki
Youichi Iino
Yusuke Ichikawa
Yoshikazu Iwase
Yasufumi Shiroyama
Kennori Kanayama
Yoshiyuki Tsubokura
Kazuki Shigemori
Kenji Ando
Hidehiko Ichikawa
Yoshie Sakurada
Yosuke Kawasaki
Youichi Iino
Yusuke Ichikawa
Yoshikazu Iwase
Yasufumi Shiroyama
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