CAS 262368-30-9

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

Codes：NINT-008

Application context (from source-drug indications)

系统性硬化相关肺间质疾病乙磺酸尼达尼布特发性肺纤维化乙磺酸尼达尼布非小细胞肺癌乙磺酸尼达尼布肺纤维化乙磺酸尼达尼布间质性肺疾病乙磺酸尼达尼布遗传性出血性毛细血管扩张乙磺酸尼达尼布

Source drugs (routes using this intermediate)

Drug	Tier	Expiry
乙磺酸尼达尼布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.

乙磺酸尼达尼布原研路线steps: 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

乙磺酸尼达尼布优化路线steps: 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

乙磺酸尼达尼布优化路线steps: 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

乙磺酸尼达尼布工艺路线steps: 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

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

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