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US 8,076,505 B2Granted
Process of preparing derivatives of 1-(2-halobiphenyl-4-yl)-cyclopropanecarboxylic acid
AssigneeChiesi Farmaceutici S.p.A.
InventorsBenoit Folleas, Hubert Botte, Thomas Delacroix, Fausto Pivetti
Life of this patent
Estimating the term…
Abstract
Compounds represented by formula (I): may be conveniently prepared by a process in which a Suzuki reaction is performed as an early step.
Claims14
A process for preparing a compound represented by formula (Ia) or a pharmaceutically acceptable salt thereof:
- said process comprising:
- (i) reacting a compound represented by formula (IIa):
- wherein X′ is selected from the group consisting of chlorine, bromine, iodine, and a triflate group, with a compound represented by formula (IIIa):
- to obtain a compound represented by formula (IVa):
- (ii) submitting said compound represented by formula (IVa) to radical bromination to obtain a compound of formula (Va):
- (iii) transforming said compound represented by formula (Va) into a nitrile compound represented by formula (VIa):
- (iv) reacting said compound represented by formula (VIa) with 1,2-dibromoethane to obtain a compound represented by formula (VIIa):
- (v) hydrolyzing said compound represented by formula (VIIa) to obtain said compound represented by formula (Ia) or a pharmaceutically acceptable salt thereof.
5 more elements
The compound 1-(3′,4′-dichloro-2-fluoro[1,1′-biphenyl]-4-yl)-cyclopropanenitrile or a salt thereof.
Dependencies are inferred from the claim text.