Back to results
US 12,240,797 B2Granted
Method of preparing a DON prodrug from L-glutamic acid
AssigneeDracen Pharmaceuticals, Inc.
InventorsJon Philip Lawson, Robert Christian Wild, Yiyang Shao, Jinchao Weng, Pavel Majer, Ivan Šnajdr, Martin Hadzima, Lukáš Tenora, Jinxiao Chu
Life of this patent
Estimating the term…
Abstract
The present disclosure provides methods of preparing a compound of Formula (I): wherein R1, R2, and R3 are as defined as set forth in the application. In one embodiment, a compound of Formula (I) is prepared in >95% chemical purity and >95% enantiomeric excess.
Claims20
A method of preparing a compound of Formula I:
- the method comprising:
- (a) reacting a compound of Formula II:
- with diazomethane in a solvent at a temperature of about −78° C. to about 0° C., wherein:
- X1 is selected from the group consisting of halogen, benzotriazole,
- R1 is C1-C4 alkyl;
- R2 is C1-C4 alkyl;
- R3 is selected from the group consisting of C1-C6 alkyl, (aryl)alkyl, and (heteroaryl)alkyl;
- R4a is selected from the group consisting of C1-C8 alkyl and C3-C8 cycloalkyl;
- and
- R4b is selected from the group consisting of C1-C8 alkyl and —CF3.
7 more elements
Dependencies are inferred from the claim text.