Partial and full agonists of A1 adenosine receptors
AssigneeCV Therapeutics, Inc.
InventorsJeff Zablocki, Elfatih Elzein, Michael Organ, Yaroslav Bilokin, Stanislas Mayer, Anthony Disanti, Scott Miller, Peter Kernast
Life of this patent
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Abstract
Disclosed are syntheses suitable for large scale manufacture of novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.
Claims25
A process for the preparation of a compound of Formula I:
- in which R is optionally substituted phenyl;
- comprising:
- contacting a compound of the formula:
- with a compound of the formula RSH in the presence of potassium carbonate in an inert solvent.
A process for the preparation of a compound of formula:
- comprising;
- contacting a compound of the formula:
- with a compound of the formula:
A process for the preparation of a compound of the formula:
- comprising:
- contacting a compound of the formula:
- with a base.
A process for the preparation of a compound of the formula:
- comprising:
- contacting a compound of the formula:
- with thionyl chloride in the presence of a base.
A process for the preparation of a compound of Formula I:
- wherein R is optionally substituted phenyl:
- comprising the steps of:
- (a) contacting a compound of the formula (1):
- with thionyl chloride in the presence of a base;
- (b) contacting the product of step (a) with a base to form a compound of formula (13):
- (c) contacting the product of step (b) with 2-hydroxycyclopentylamine in the presence of a base to provide a compound of formula (5);
- and;
- (d) contacting the product of step (c) with a compound of the formula RSH in the presence of a base, in which R is as defined above.
Dependencies are inferred from the claim text.