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US 6,747,158 B2Granted
Efficient process for the preparation of a factor Xa inhibitor
AssigneeBristol-Myers Squibb Pharma Company
InventorsHui-Yin Li, Luigi Anzalone, Fuqiang Jin, David J. Meloni, Jung-Hui Sun, Lucius T. Rossano, Christopher A. Teleha, Jiacheng Zhou, Thomas E. Smyser
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Abstract
The present invention relates to the process for the preparation of the compound of Formula I: from its corresponding 3-cyano-4-fluorophenyl-pyrazole and intermediates useful therein.
Claims25
A process for making a compound of Formula II:
- comprising:
- (a) converting the compound of Formula VI to its corresponding hydrazine and contacting the hydrazine of Formula VI with a compound of Formula VII in the presence of MeOH to form a compound of Formula VIII;
- and,
- (a1) converting a compound of Formula VIII to a compound of Formula II.
1 more element
A process for making a compound of Formula II:
- comprising:
- (a) converting the compound of Formula VI to its corresponding hydrazine and contacting the hydrazine of Formula VI with a compound of Formula VII to form a compound of Formula VIII;
- and,
- (a1) contacting a compound of Formula VIII with an oxidant to form a compound of Formula II, wherein the oxidant is selected from KMnO4 and NaClO2.
1 more element
A process for making a compound of Formula II:
- comprising:
- (a) converting the compound of Formula VI to its corresponding hydrazine and contacting the hydrazine of Formula VI with a compound of Formula VII to form a compound of Formula VIII;
- and,
- (a1) contacting a compound of Formula VIII with an oxidant in the presence of a buffer to form a compound of Formula II.
1 more element
Dependencies are inferred from the claim text.