Thyroid hormone receptor agonist and use thereof
View Patent ↗A thyroid hormone receptor agonist and its use in the treatment of a disease associated thyroid hormone receptor beta are described. The compound can be effective in lowering cholesterol with minimum or no adverse effects on the heart or thyroid hormone axis.
1. A method comprising:
(a) reacting a compound of (I-A)
with paraformaldehyde to form a compound of (I-B)
(b) reacting the compound of (I-B)
and R 2 Cl to form a compound of (I-C)
(c) reacting the compound of (I-C)
with a compound of (I-E)
to form a compound of (I-F)
(d) reacting the compound of (I-F)
with 2-benzylphenol to form a compound of (I-G)
(e) deprotecting the compound of formula (I-G)
to form a compound of (I-I)
wherein each R 1 is independently a protecting group for hydroxyl group and R 2 is a leaving group.
2. The method of claim 1 , comprising reacting the compound of (I-I)
with iodomethyl pivalate to form a compound of Formula I
3. The method of claim 1 , comprising converting chloromethyl pivalate to iodomethyl pivalate.
4. The method of claim 1 , comprising reacting 3,5-dimethylphenol with formaldehyde to form the compound of compound of (I-E)
5. The method of claim 1 , wherein R 1 is isopropyl.
6. The method of claim 1 , wherein R 2 is tosyl.