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US 9,315,455 B2Granted
Process for isomerizing fused bicyclic structures and preparation of vitamin D analogs comprising the same
AssigneeHybrigenics
InventorsJean-Luc Moutou, Florent Mouton, Gilles Pellegrino, Jean Lafay
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Abstract
The present invention concerns a process of isomerizing trans fused bicyclic derivatives into cis fused bicyclic derivatives and the preparation of vitamin D or analogs thereof comprising said isomerization step.
Claims8
A process of preparation of inecalcitol of formula:
- said process comprising the process of preparation of a cis fused bicyclic compound of formula (II) from a corresponding trans fused bicyclic compound of formula (I):
- said process comprising the step of reacting said trans fused bicyclic compound with an hydride base which is NaH or KH,
- wherein in formulae (I) and (II):
- m=n=0,
- R1=methyl,
- R2=H;
- and
- R3 is of formula:
- where X is H or X is a protective group of the OH function, and the broken bond is the bond of the cyclopentyl core;
- and said process of preparation of the compound of formula (II) being followed by the transformation of said compound of formula (II) into inecalcitol in one or more steps.
7 more elements
Dependencies are inferred from the claim text.