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US 11,691,946 B2Granted
Preparation of Trifarotene and intermediates and polymorphs thereof
AssigneeTaro Pharmaceutical Industries Ltd.
InventorsIlana Ozer, Yulia Kaftanov, Elliot Simhon, Andrey Dushkin, Shani Sheffer Dee-Noor, Hillel Pizem, Avi Avramoff
Life of this patent
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Abstract
The present disclosure provides a process for the preparation of Trifarotene. The disclosure also provides novel intermediates in the process described herein. Also provided are novel polymorphs of Trifarotene.
Claims20
A process for the preparation of a compound of formula (I) [Trifarotene], or a salt thereof
- comprising hydrolyzing a compound of formula (V)
- wherein R4 is hydrogen, a substituted or unsubstituted linear or branched C1-C8 alkanoyl group, a substituted or unsubstituted linear or branched C2-C8 alkenoyl group, a substituted or unsubstituted linear or branched C2-C8 alkynoyl group, a substituted or unsubstituted cycloalkanoyl group, a substituted or unsubstituted aryl carbonyl group, a substituted or unsubstituted heterocyle carbonyl group, a substituted or unsubstituted heteroaryl carbonyl group, or a C1-C8 alkanoyl group wherein one or more carbons in the C1-C8 alkanoyl group is replaced by one or more heteroatoms;
- and
- wherein Y is a nitrile (CN) or amide (CONH2);
- to obtain the compound of formula (I).
2 more elements
A compound of formula (V)
- wherein R4 is hydrogen, a substituted or unsubstituted linear or branched C1-C8 alkanoyl group, a substituted or unsubstituted linear or branched C2-C8 alkenoyl group, a substituted or unsubstituted linear or branched C2-C8 alkynoyl group, a substituted or unsubstituted cycloalkanoyl group, a substituted or unsubstituted aryl carbonyl group, a substitute or unsubstituted heterocyle carbonyl group, a substituted or unsubstituted heteroaryl carbonyl group, or a C1-C8 alkanoyl group wherein one or more carbons in the C1-C8 alkanoyl group is replaced by one or more heteroatoms;
- and
- wherein Y is a nitrile (CN) or amide (CONH2).
Dependencies are inferred from the claim text.