CAS 172732-52-4

2-(1,3,2-dioxaborinan-2-yl)benzonitrile

Codes：PERAM-006

Application context (from source-drug indications)

强直阵挛性癫痫吡仑帕奈癫痫部分性发作吡仑帕奈癫痫吡仑帕奈癫痫发作吡仑帕奈

Source drugs (routes using this intermediate)

Drug	Tier	Expiry
吡仑帕奈Perampanel Hydrate	Tier C — Watch / trade	2028

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.

吡仑帕奈原研路线steps: 6total yield: /

5-bromopyridin-2-amine→5-bromo-3-iodopyridin-2-amine→5-bromo-3-iodopyridin-2(1H)-one→phenylboronic acid→5-bromo-3-iodo-1-phenylpyridin-2(1H)-one→2-(1,3,2-dioxaborinan-2-yl)benzonitrile→2-(5-bromo-2-oxo-1-phenyl-1,2-dihydropyridin-3-yl)benzonitrile→2-(2-oxo-1-phenyl-5-(tributylstannyl)-1,2-dihydropyridin-3-yl)benzonitrile→2-chloropyridine

吡仑帕奈优化路线steps: 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

吡仑帕奈优化路线steps: 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

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