Methods of manufacturing bioactive 3-esters of betulinic aldehyde and betulinic acid
OwnerPavel A. Krasutsky, Oksana Kolomitsynainventors
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Abstract
The present invention provides a method for preparing a compound of formula (I), the method comprising contacting a compound of formula (II) with an effective amount of a compound of formula (III) or (IV). The present invention also provides a method for preparing a compound of formula (VI), the method comprising contacting a compound of formula (II) with an effective amount of one or more of 2,2-dimethylsuccinic acid, 2,2 dimethylbutanedioyl dichloride, 2,2-dimethylbutanedioyl dibromide, and 2,2 dimethylsuccinic anhydride. The present invention also provides a compound obtained from the method of the present invention.
Claims25
A method for preparing a compound of formula (I):
- the method comprising contacting a compound of formula (II):
- with an effective amount of a compound of formula (III) or (IV):
- wherein,
- R1 is X1C(═O)Rx—;
- Rx is alkylene, cycloalkylene, carbocyclene, arylene, heterocyclene, or heteroarylene;
- X1 is hydroxyl, halo, alkoxy or —OC(═O)Ry;
- Ry is alkyl, cycloalkyl, carbocycle, aryl, heterocycle, or heteroaryl;
- each of R2-R5 is independently H, alkyl, cycloalkyl, carbocycle, aryl, heterocycle, or heteroaryl;
- and
- the bond represented by — is optionally present.
3-25. (canceled)
27-35. (canceled)
A method for preparing a compound of formula (VI):
- the method comprising contacting a compound of formula (II):
- with an effective amount of a compound selected from the group of 2,2-dimethylsuccinic acid, 2,2-dimethylbutanedioyl dichloride, 2,2-dimethylbutanedioyl dibromide, and 2,2-dimethylsuccinic anhydride;
- wherein the bond represented by — is optionally present.
(canceled)
39-42. (canceled)
47-48. (canceled)
Dependencies are inferred from the claim text.