Process for the preparation of aniline-derived thyroid receptor ligands
0 Assignments
0 Petitions
Accused Products
Abstract
Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.
-
Citations
38 Claims
-
1-30. -30. (canceled)
-
31. A compound of formula IIIA
R2 and R3 independently represent bromo, chloro, or methyl; - and R4 represents hydrogen or methyl.
- View Dependent Claims (32, 33)
-
34. A process for the synthesis of a phenol of formula A
wherein: -
G is a protecting group; and R1 represents halogen, trifluoromethyl, an alkyl group of 1 to 6 carbons, or a cycloalkyl group of 3 to 7 carbons; comprising the steps of; a) reacting an aldehyde of formula A-I with MHSO3 to form a sulfonate of formula A-II wherein M is a metal; and b) reacting the sulfonate of formula A-II with an oxidant, in the presence of a proton source, to form the phenol of formula A above.
-
-
35. A compound selected from the group consisting of compounds of formula A-I and formula A-II,
wherein G represents a protecting group; - M represents a metal; and
R.sup.1 represents halogen, trifluoromethyl, an alkyl group of 1 to 6 carbons, or a cycloalkyl group of 3 to 7 carbons. - View Dependent Claims (36, 37)
- M represents a metal; and
-
38. A compound of formula A
wherein G represents a protecting group; - and
R1 represents halogen, trifluoromethyl, an alkyl group of 1 to 6 carbons, or a cycloalkyl group of 3 to 7 carbons; with the proviso that, when G is a methyl group, R1 is not a member of the group consisting of bromo, chloro, iodo, t-butyl, cyclohexyl, cyclopentyl, and isopropyl.
- and
Specification