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US 6,610,858 B2Granted
Efficient method for the conversion of nitriles to amidines
AssigneeBristol-Myers Squibb Pharma Company
InventorsPhilip Ma, Pasquale N. Confalone, Hui-Yin Li
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Abstract
The present invention relates to processes for the conversion of nitriles to amidines in the preparation of compounds which are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex. The compounds described herein are potent thrombolytics and useful for the inhibition of platelet aggregation in the treatment of thromboembolic disorders.
Claims10
A process for the formation of a compound of the formula (I):
- or a pharmaceutically acceptable salt form thereof;
- wherein:
- R1 is selected from H or NHC(═O)—O—R1b;
- R1b is selected from C1-8 alkyl;
- R2 is H;
- R3 and R4 are H;
- R5 is selected from the group consisting of:
- hydroxy, C1-C10 alkoxy;
- said process comprising:
- reacting a compound of formula (IV):
- wherein:
- R6 is selected from the group consisting of C1-C8 alkyl;
- with hydrogen under a suitable pressure in the presence of a hydrogenation catalyst to form a compound of formula (I) or a pharmaceutically acceptable salt form thereof.
10 more elements
Dependencies are inferred from the claim text.