CAS 56341-41-4

5-fluoroindolin-2-one

Codes: SUNT-009, VORO-001

Application context (from source-drug indications)

Pancreatic neuroendocrine tumourSunitinib MalateRenal cell carcinomaSunitinib MalateGastrointestinal stromal tumourSunitinib MalateOsteosarcomaSunitinib MalateSarcomaSunitinib MalateLymphomaSunitinib MalateRenal cell carcinomaVorolanibDiabetic macular oedemaVorolanib湿性年龄相关性黄斑变性VorolanibDiabetic retinopathyVorolanib肾肿瘤VorolanibHepatic function declineVorolanib

Source drugs (routes using this intermediate)

Drug	Tier	Expiry
Sunitinib Malate	Tier B — Position early	-
Vorolanib	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.

Sunitinib MalateOriginator routesteps: 6total yield: 216 g

4-methyleneoxetan-2-one→N1,N1-diethylethane-1,2-diamine→N-(2-(diethylamino)ethyl)-3-oxobutanamide→tert-butyl 3-oxobutanoate→tert-butyl 4-((2-(diethylamino)ethyl)carbamoyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate→N-(2-(diethylamino)ethyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide→N-(chloromethylene)-N-methylmethanaminium chloride→N-(2-(diethylamino)ethyl)-5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxamide→5-fluoroindolin-2-one→(S)-2-hydroxysuccinic acid

Sunitinib MalateProcess routesteps: 8total yield: 1.7 kg

N1,N1-diethylethane-1,2-diamine→tert-butyl 3-oxobutanoate→N-(2-(diethylamino)ethyl)-5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxamide→5-fluoroindolin-2-one→(S)-2-hydroxysuccinic acid→(E)-tert-butyl 2-(hydroxyimino)-3-oxobutanoate→ethyl 3-oxobutanoate→2-(tert-butyl) 4-ethyl 3,5-dimethyl-1H-pyrrole-2,4-dicarboxylate→ethyl 2,4-dimethyl-1H-pyrrole-3-carboxylate→ethyl 5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylate→5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid

Sunitinib MalateOptimised routesteps: 6total yield: 12 g

N1,N1-diethylethane-1,2-diamine→5-fluoroindolin-2-one→(S)-2-hydroxysuccinic acid→ethyl 3-oxobutanoate→ethyl 5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylate→diethyl 3,5-dimethyl-1H-pyrrole-2,4-dicarboxylate→4-(ethoxycarbonyl)-3,5-dimethyl-1H-pyrrole-2-carboxylic acid→ethyl (Z)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxylate

VorolanibOriginator routesteps: 3total yield: 20 mg

5-fluoroindolin-2-one→5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid→(Z)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic acid→3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl (Z)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxylate→(S)-3-amino-N,N-dimethylpyrrolidine-1-carboxamide→(S,Z)-N-(1-(dimethylcarbamoyl)pyrrolidin-3-yl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide

Intermediates available on this site

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Supplier	Product	Price band	MOQ	Lead time	Qualifications	Action
Qualified Partner — East China API Works	5-Fluoro-2-oxindole Pharmaceutical Intermediates	On request	On request	On request	—

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