CAS 13472-85-0

5-bromo-2-methoxypyridine

Codes: PERAM-011, FIMEP-016

Application context (from source-drug indications)

Tonic-clonic seizurePerampanel HydratePartial-onset seizurePerampanel HydrateEpilepsyPerampanel HydrateSeizurePerampanel HydrateCushing's syndromeFimepinostatGliomaFimepinostatGlioblastomaFimepinostatDiffuse intrinsic pontine gliomaFimepinostat髓母细胞瘤Fimepinostat星形细胞瘤Fimepinostat

Source drugs (routes using this intermediate)

Drug	Tier	Expiry
Perampanel Hydrate	Tier C — Watch / trade	2028
Fimepinostat	Tier C — Watch / trade	-

Position in synthesis routes (up/downstream chain)

Ordered by route registration; left → right is the synthesis direction. The highlighted node is the current CAS; others link to their own profiles.

Perampanel HydrateOptimised routesteps: 8total yield: 0.06 g

phenylboronic acid→2-(1,3,2-dioxaborinan-2-yl)benzonitrile→2,5-dibromopyridine→5-bromo-2-methoxypyridine→2-(tributylstannyl)pyridine→6'-methoxy-2,3'-bipyridine→[2,3'-bipyridin]-6'(1'H)-one→5'-bromo-[2,3'-bipyridin]-6'(1'H)-one→5'-bromo-6'-methoxy-2,3'-bipyridine→2-(6'-methoxy-[2,3'-bipyridin]-5'-yl)benzonitrile→2-(6'-oxo-1',6'-dihydro-[2,3'-bipyridin]-5'-yl)benzonitrile

Perampanel HydrateOptimised routesteps: 7total yield: 168.3 g

2-(1,3,2-dioxaborinan-2-yl)benzonitrile→5-bromo-2-methoxypyridine→6'-methoxy-2,3'-bipyridine→[2,3'-bipyridin]-6'(1'H)-one→2-methoxypyridine→2-(phenylsulfonyl)pyridine→1'-phenyl-[2,3'-bipyridin]-6'(1'H)-one→5'-bromo-1'-phenyl-[2,3'-bipyridin]-6'(1'H)-one

FimepinostatOriginator routesteps: 14total yield: 9.2 g (Fimepinostat)

methyl 3-aminothiophene-2-carboxylate→thieno[3,2-d]pyrimidine-2,4(1H,3H)-dione→FIMEP-003→FIMEP-004→2-chloro-4-morpholinothieno[3,2-d]pyrimidine-6-carbaldehyde→1-(2-chloro-4-morpholinothieno[3,2-d]pyrimidin-6-yl)-N-methylmethanamine→ethyl 2-chloropyrimidine-5-carboxylate→ethyl 2-(((2-chloro-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)(methyl)amino)pyrimidine-5-carboxylate→(6-methoxypyridin-3-yl)boronic acid→FIMEP-010→FIMEP-011→FIMEP-012→FIMEP-013→FIMEP-014→2-methoxypyridine→5-bromo-2-methoxypyridine→Fimepinostat

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