CAS 262368-30-9

N-(4-aminophenyl)-2-(4-methylpiperazin-1-yl)acetamide

Codes: NINT-008

Application context (from source-drug indications)

Systemic sclerosis-associated interstitial lung diseaseNintedanib EsylateIdiopathic pulmonary fibrosisNintedanib EsylateNon-small cell lung cancerNintedanib EsylatePulmonary fibrosisNintedanib EsylateInterstitial lung diseaseNintedanib EsylateHereditary haemorrhagic telangiectasiaNintedanib Esylate

Source drugs (routes using this intermediate)

Drug	Tier	Expiry
Nintedanib Esylate	Tier B — Position early	-

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.

Nintedanib EsylateOriginator routesteps: 7total yield: 12.4 g

methyl 3-nitrobenzoate→methyl 2-chloroacetate→methyl 4-(2-methoxy-2-oxoethyl)-3-nitrobenzoate→methyl 2-oxo-1,3-dihydroindole-6-carboxylate →methyl 1-acetyl-2-oxoindoline-6-carboxylate→(trimethoxymethyl)benzene→(Z)-methyl 1-acetyl-3-(methoxy(phenyl)methylene)-2-oxoindoline-6-carboxylate→N-(4-aminophenyl)-2-(4-methylpiperazin-1-yl)acetamide→2-bromo-N-methyl-N-(4-nitrophenyl)acetamide→1-methylpiperazine→N-methyl-2-(4-methylpiperazin-1-yl)-N-(4-nitrophenyl)acetamide

Nintedanib EsylateOptimised routesteps: 10total yield: 35.1 g

methyl 2-oxo-1,3-dihydroindole-6-carboxylate →(trimethoxymethyl)benzene→N-(4-aminophenyl)-2-(4-methylpiperazin-1-yl)acetamide→1-methylpiperazine→4-chloro-3-nitrobenzoic acid→methyl 4-chloro-3-nitrobenzoate→dimethyl malonate→dimethyl 2-(4-(methoxycarbonyl)-2-nitrophenyl)malonate→2-chloroacetic anhydride→methyl 1-(2-chloroacetyl)-2-oxoindoline-6-carboxylate→(Z)-methyl 1-(2-chloroacetyl)-3-(methoxy(phenyl)methylene)-2-oxoindoline-6-carboxylate→(Z)-methyl 3-(methoxy(phenyl)methylene)-2-oxoindoline-6-carboxylate→ethanesulfonic acid→N-methyl-4-nitroaniline→2-chloroacetyl chloride→2-chloro-N-methyl-N-(4-nitrophenyl)acetamide

Nintedanib EsylateOptimised routesteps: 3total yield: 2.37 g

methyl 4-(2-methoxy-2-oxoethyl)-3-nitrobenzoate→(trimethoxymethyl)benzene→N-(4-aminophenyl)-2-(4-methylpiperazin-1-yl)acetamide→(Z)-methyl 4-(1,3-dimethoxy-3-oxo-1-phenylprop-1-en-2-yl)-3-nitrobenzoate→(Z)-methyl 4-(3-methoxy-1-((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)-3-oxo-1-phenylprop-1-en-2-yl)-3-nitrobenzoate

Nintedanib EsylateProcess routesteps: 2total yield: 538 g

methyl 2-oxo-1,3-dihydroindole-6-carboxylate →N-(4-aminophenyl)-2-(4-methylpiperazin-1-yl)acetamide→ethanesulfonic acid→methyl benzoate

Intermediates available on this site

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Supplier	Product	Price band	MOQ	Lead time	Qualifications	Action
Unibest Nantong cGMP Site	N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin -1-yl)acetamide Pharmaceutical Intermediates	On request	On request	On request	—

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