A Short Synthesis of the Factor‐Xa Inhibitor DX‐9065a using palladium‐catalyzed key steps | Zendy

Kehr Christiane | Zendy; Neidlein Richard | Zendy; Engh Richard A. | Zendy; Brandsretter Hans | Zendy; Kucznierz Ralf | Zendy; Leinert Herbert | Zendy; Marzenell Klaus | Zendy; Strein Klaus | Zendy; Saal Wolfgang Von Der | Zendy

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A Short Synthesis of the Factor‐Xa Inhibitor DX‐9065a using palladium‐catalyzed key steps

Author(s) -

Kehr Christiane,

Neidlein Richard,

Engh Richard A.,

Brandsretter Hans,

Kucznierz Ralf,

Leinert Herbert,

Marzenell Klaus,

Strein Klaus,

Saal Wolfgang Von Der

Publication year - 1997

Publication title -

helvetica chimica acta

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.74

H-Index - 82

eISSN - 1522-2675

pISSN - 0018-019X

DOI - 10.1002/hlca.19970800322

Subject(s) - chemistry , cyanation , trifluoromethanesulfonate , palladium , catalysis , cleavage (geology) , stereochemistry , medicinal chemistry , total synthesis , organic chemistry , geotechnical engineering , fracture (geology) , engineering

We describe a new, efficient synthesis of DX‐9065a ( 4 ), a potent inhibitor of the blood coagulation enzyme factor Xa (fXa) which has previously been prepared in more than 20 steps. We saved approximately 10 steps starting with a Pd‐catalyzed cyanation of the triflate 10 of 7‐methoxynaphthalen‐2‐ol ( 9 ). After cleavage of the MeO group with boron tribromide, the triflate 6 was coupled to acrylate 5 in a Heck reaction (→3). The subsequent transformations led to DX‐9065 a.

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