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US 8,524,907 B2Granted
Methods of synthesizing pharmaceutical salts of a factor Xa inhibitor
AssigneeMillennium Pharmaceuticals, Inc.
InventorsRobert M. Scarborough, James P Kanter, Keiko Sujino, Sharique Sami Zuberi
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Abstract
Novel methods of preparing a compound of Formula I which is an inhibitor of Factor Xa and its maleate salt, are described herein.
Claims23
A method of preparing a compound of Formula I
- or a salt thereof, which method comprises contacting LiN(CH3)2 with a compound of Formula F:
- or a salt thereof, under conditions to form the compound of Formula I, and optionally contacting the compound of Formula I with an organic or inorganic acid to form a salt of the compound of Formula I.
A method of preparing a compound of Formula I:
- or a salt thereof, comprising:
- a) contacting a compound of Formula A:
- with a compound of Formula B:
- under reaction conditions comprising acetonitrile as a solvent to form a compound of Formula C:
- b) exposing the compound of Formula C to reaction conditions to form a compound of Formula D:
- c) contacting the compound of Formula D with a compound of Formula E:
- under reaction conditions to form a compound of Formula F:
- or a salt thereof;
- and
- d) contacting LiN(CH3)2 with the compound of Formula F or a salt thereof, under reaction conditions to form the compound of Formula I, and optionally contacting the compound of Formula I with an organic or inorganic acid to form a salt of the compound of Formula I.
7 more elements
Dependencies are inferred from the claim text.