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US 12,275,696 B2Granted
Process for preparing tapinarof
AssigneeDermavant Sciences GmbH
InventorsIan Paul Andrews, Nicholas Calandra, Tyler Andrew Davis, Ravinder Reddy Sudini
Life of this patent
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Abstract
The present invention provides processes for the preparation of 3, 5-Dihydroxy-4-isopropyl-trans-stilbene or a salt or solvate thereof and novel intermediates used therein. In some embodiments the 3, 5-Dihydroxy-4-isopropyl-trans-stilbene is prepared from (E)-2-chloro-2-isopropyl-5-styrylcyclohexane-1,3-dione. Also disclosed are crystal forms of 3, 5-Dihydroxy-4-isopropyl-trans-stilbene or a salt or solvate thereof and pharmaceutical compositions comprising same.
Claims18
A process for the preparation of a compound of Formula (I) or a salt or solvate thereof
- comprising one or more of the process steps (a), (b) and (c) wherein:
- (a) comprises (i) reaction of a compound of Formula (III) or a salt thereof
- to form a compound of Formula (II) or a salt thereof
- wherein X is Cl, Br, or I, and thereafter (ii) conversion of the compound of Formula (II) or a salt thereof into the compound of Formula (I) or a salt or solvate thereof;
- (b) comprises conversion of a compound of Formula (VI) or a salt thereof
- into a compound of Formula (III) or a salt thereof
- and thereafter conversion of the compound of Formula (III) or a salt thereof into a compound of Formula (I) or a salt or solvate thereof;
- and
- (c) comprises conversion of a compound of Formula (IX) or a salt thereof
- into a compound of Formula (VI) or a salt thereof
- and thereafter conversion of the compound of Formula (VI) or a salt thereof into a compound of Formula (I) or a salt or solvate thereof.
8 more elements
Dependencies are inferred from the claim text.