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US 6,645,975 B1Granted
Process for the preparation of dinaposoline
AssigneePurdue Research Foundation
InventorsSing-Yuen Sit, Swanee E. Jacutin-Porte
Life of this patent
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Abstract
The present invention relates to a novel process for the preparation of compounds of the formula wherein R1, R2, R4, R5, R6 and A are as defined herein, and to certain derivations of Formula IX which are useful for the treatment of movement disorders.
Claims13
A process for preparing a compound of the formula
- wherein R1 and R2 each are hydrogen;
- A is CH2, CHOH or C═O;
- R is hydrogen or C1-4alkyl;
- and R4, R5 and R6 each are independently hydrogen, C1-4alkyl, C1-4alkoxy, hydroxy or halogen, comprising the steps of (a) reducing a compound of the formula
- wherein R1 and R2 each are a hydroxy-protecting group;
- or R1 and R2 may be joined together to form —(CH2)n— in which n is 1 to 3 and R4, R5 and R6 and A are as defined above;
- with a reducing agent and (b) deprotecting the resulting reduced product to produce the compound of Formula IX wherein R1 and R2 are hydrogen and (c) optionally, alkylating the product of step (a) or (b) to produce a compound of Formula IX wherein R is C1-4alkyl.
4 more elements
A compound of the formula
- wherein
- R1 and R2 each are hydrogen or a hydroxy-protecting group;
- or R1 and R2 may be joined together to form —(CH2)n—,
- n is 1 to 3;
- A is CHOR1 or C═O;
- R is hydrogen or C1-4alkyl;
- and
- R4, R5
- and R6 each are independently hydrogen, C1-4alkyl, C1-4alkoxy, hydroxy or halogen.
6 more elements
Dependencies are inferred from the claim text.