CAS 619-67-0

4-hydrazinylbenzoic acid

Codes：DEFE-004、DEFE-010

Application context (from source-drug indications)

地中海贫血地拉罗司铁超负荷地拉罗司β-地中海贫血地拉罗司造血干细胞移植地拉罗司骨髓增生异常综合征地拉罗司贫血地拉罗司

Source drugs (routes using this intermediate)

Drug	Tier	Expiry
地拉罗司Deferasirox	Tier B — Position early	-

Position in synthesis routes (up/downstream chain)

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地拉罗司原研路线steps: 2total yield: /

2-hydroxybenzoyl chloride→2-hydroxybenzamide→2-(2-hydroxyphenyl)-4H-benzo[e][1,3]oxazin-4-one→4-hydrazinylbenzoic acid

地拉罗司优化路线steps: 4total yield: 22.8 g

2-(benzyloxy)benzonitrile→methyl 2-(benzyloxy)benzimidate hydrochloride→methyl 2-(benzyloxy)benzimidate→2-hydroxybenzoyl chloride→2-(2-(benzyloxy)phenyl)-4H-benzo[e][1,3]oxazin-4-one→4-hydrazinylbenzoic acid

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