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US 5,633,373 AGranted
Enantioselective synthesis of antifolates
AssigneeEli Lilly and Company
InventorsCharles J. Barnett, Thomas M. Wilson
Life of this patent
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Abstract
A process and intermediates for the enantioselective synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid are disclosed.
Claims3
A process for preparing a compound of the formula ##STR11## wherein E is hydroxy or amino;
- n is 0 or 1;
- E.sup.8 is a carboxy-protecting group;
- and the carbon marked * is substantially pure R or S configuration;
- comprising reacting a compound of the formula ##STR12## wherein E.sup.1 is hydroxy;
- with a triazine of the formula ##STR13## wherein the E.sup.7 groups independently are chloro, methoxy or phenoxy;
- and then with a L-glutamate of the formula ##STR14## in the presence of N-methylmorpholine.
3 more elements
Dependencies are inferred from the claim text.