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US 2010/0137602 A1Published application
Process and intermediates for preparing arzoxifene
AssigneeEli Lilly and Company
InventorsCharles Arthur Alt, Douglas Patton Kjell, Tony Yantao Zhang, Fu-Yao Zhang, Jared Wade Fennell, Kevin Dale Siebert
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Abstract
The present invention provides for novel compounds of formula I wherein X is S or S(O); R1 and R2 are each independently selected from the group consisting of —CH2CH3 and phenyl; or R1 and R2 combine to form morpholino; and processes to prepare arzoxifene.
Claims16
A compound of the formula:
- wherein
- X is S or S(O);
- R1 and R2 are each independently selected from the group consisting of —CH2CH3 and phenyl;
- or R1 and R2 combine to form morpholino.
1 more element
A compound that is diethyl-carbamic acid 2-(4-methoxy-phenyl)-3-[4-(2-piperidin-1-yl-ethoxy)-phenoxy]-benzo[b]thiophen-6-yl ester.
A process for preparing arzoxifene comprising:
- a) reducing an intermediate sulfoxide compound of the formula:
- to form a compound of the formula:
- wherein R1 and R2 are each independently selected from the group consisting of —CH2CH3 and phenyl;
- or R1 and R2 combine to form morpholino;
- and
- b) deprotecting the sulfide compound to form arzoxifene.
3 more elements
Dependencies are inferred from the claim text.