Back to results
US 10,414,791 B2Granted
Methods for preparation of bile acids and derivatives thereof
AssigneeIntercept Pharmaceuticals, Inc.
InventorsRoberto Pellicciari, Antimo Gioiello
Life of this patent
Estimating the term…
Abstract
The present application relates to a method of preparing compounds of Formula (I) or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, R1 is H, α-OH, β-OH, or an oxo group.
Claims20
A method of preparing a compound of Formula (I):
- or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R1 is H, α-OH, β-OH, or an oxo group, from compound 2 comprising the steps of:
- (1) converting compound 2 to compound 5
- (2) converting compound 5 into compound 6:
- (3) converting compound 6 into compound 9:
- (4) converting compound 9 into compound 10
- (5) alkylating compound 10 regioselectively and stereoselectively to yield compound 11
- wherein P1 is a protecting group or H;
- (6) regioselectively and stereoselectively reducing compound 11 to yield compound
- wherein P2 is a protecting group;
- and
- (7) selectively reducing compound 13 and deprotecting to yield the compound of Formula (I), wherein R1 is H;
- or
- (8) oxidizing compound 13 regioselectively to yield compound 15
- and
- (9) selectively reducing compound 15 and deprotecting to yield the compound of Formula (I), wherein R1 is α-OH, β-OH, or an oxo group.
12 more elements
Dependencies are inferred from the claim text.