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举例 :可输入Filippa Pettersson 或者 Cancer Res. 75(6) , 1102-12, (2015) 或者10.1002/anie.201600521

Synthesis and neuroleptic activity of N-[(1-ethyl-2-pyrrolidinyl) methyl]-2-methoxy-5-sulfonamidobenzamides

M Ogata, H Matsumoto, S Kida, T Shiomi…

文献索引：Ogata, Masaru; Matsumoto, Hiroshi; Kida, Shiro; Shiomi, Teruo; Eigyo, Masami; Hirose, Katsumi Journal of Medicinal Chemistry, 1984 , vol. 27, # 9 p. 1137 - 1141

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被引用次数: 3

摘要

A series of some novel N-[(l-ethyl-2-pyrrolidinyl) methyl] benzamides involving replacement of the sulfarnoyl group in sulpiride with a sulfonamido group was synthesized and tested for dopamine receptor blockade. In comparison with sulpiride, several compounds were considerably more potent than sulpiride as dopamine receptor blockers. The structure- activity relationships are discussed.

N-乙基-2-氨甲基吡咯烷结构式

N-乙基-2-氨甲基吡咯烷

~%

4-chloro-N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-(sulfamoylamino)benzamide结构式

4-chloro-N-[(1-...

4-Chloro-2-Methoxy-5-nitro-benzoic acid结构式

4-Chloro-2-Meth...

~%

4-chloro-N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-(sulfamoylamino)benzamide结构式

4-chloro-N-[(1-...

N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxy-4-chloro-5-aminobenzamide结构式

N-[(1-ethyl-2-p...

~%

4-chloro-N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-(sulfamoylamino)benzamide结构式

4-chloro-N-[(1-...

N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxy-4-chloro-5-nitrobenzamide结构式

N-[(1-ethyl-2-p...

~%

4-chloro-N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-(sulfamoylamino)benzamide结构式

4-chloro-N-[(1-...

Benzoyl chloride, 4-chloro-2-methoxy-5-nitro结构式

Benzoyl chlorid...

~%

4-chloro-N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-(sulfamoylamino)benzamide结构式

4-chloro-N-[(1-...

N-(1-ethyl-2-pyrrolidinylmethyl)-2-methoxy-4-chloro-5-t-butylaminosulfonamidobenzamide结构式

N-(1-ethyl-2-py...

~28%

4-chloro-N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-(sulfamoylamino)benzamide结构式

4-chloro-N-[(1-...

2-Methoxy-4-Methyl-5-nitro-benzoic acid结构式

2-Methoxy-4-Met...

~%

2-甲氧基-4-甲基-5-硝基苯甲酸甲酯结构式

2-甲氧基-4-甲基-5-硝基苯甲酸甲酯

甲基氨基磺酰氯结构式

甲基氨基磺酰氯

N-(1-ethyl-2-pyrrolidinylmethyl)-2-methoxy-5-aminobenzamide结构式

N-(1-ethyl-2-py...

~56%

N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-(methylsulfamoylamino)benzamide结构式

N-[(1-ethylpyrr...

2-甲氧基-5-硝基苯甲酸结构式

2-甲氧基-5-硝基苯甲酸

~%

N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-(methylsulfamoylamino)benzamide结构式

N-[(1-ethylpyrr...

2-Methoxy-5-nitrobenzoyl chloride结构式

2-Methoxy-5-nit...

~%

N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-(methylsulfamoylamino)benzamide结构式

N-[(1-ethylpyrr...

N-(1-ethyl-2-pyrrolidinylmethyl)-2-methoxy-5-nitrobenzamide结构式

N-(1-ethyl-2-py...

~%

N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-(methylsulfamoylamino)benzamide结构式

N-[(1-ethylpyrr...

N-乙基-2-氨甲基吡咯烷结构式

N-乙基-2-氨甲基吡咯烷

~%

4-chloro-N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-[methyl(sulfamoyl)amino]benzamide结构式

4-chloro-N-[(1-...

4-Chloro-2-Methoxy-5-nitro-benzoic acid结构式

4-Chloro-2-Meth...

~%

4-chloro-N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-[methyl(sulfamoyl)amino]benzamide结构式

4-chloro-N-[(1-...

N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxy-4-chloro-5-aminobenzamide结构式

N-[(1-ethyl-2-p...

~%

4-chloro-N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-[methyl(sulfamoyl)amino]benzamide结构式

4-chloro-N-[(1-...

N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxy-4-chloro-5-nitrobenzamide结构式

N-[(1-ethyl-2-p...

~%

4-chloro-N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-[methyl(sulfamoyl)amino]benzamide结构式

4-chloro-N-[(1-...

Benzoyl chloride, 4-chloro-2-methoxy-5-nitro结构式

Benzoyl chlorid...

~%

4-chloro-N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-[methyl(sulfamoyl)amino]benzamide结构式

4-chloro-N-[(1-...

4-chloro-N-((1-ethylpyrrolidin-2-yl)methyl)-2-methoxy-5-(methylamino)benzamide结构式

4-chloro-N-((1-...

~%

4-chloro-N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-[methyl(sulfamoyl)amino]benzamide结构式

4-chloro-N-[(1-...

4-chloro-N-((1-ethylpyrrolidin-2-yl)methyl)-2-methoxy-5-(2,2,2-trifluoroacetamido)benzamide结构式

4-chloro-N-((1-...

~%

4-chloro-N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-[methyl(sulfamoyl)amino]benzamide结构式

4-chloro-N-[(1-...

5-((N-(tert-butyl)sulfamoyl)(methyl)amino)-4-chloro-N-((1-ethylpyrrolidin-2-yl)methyl)-2-methoxybenzamide结构式

5-((N-(tert-but...

~%

4-chloro-N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-[methyl(sulfamoyl)amino]benzamide结构式

4-chloro-N-[(1-...

2-甲氧基-4-甲基-5-硝基苯甲酸甲酯结构式

2-甲氧基-4-甲基-5-硝基苯甲酸甲酯

~%

5-氨基-2-甲氧基-4-甲基苯甲酸甲酯结构式

5-氨基-2-甲氧基-4-甲基苯甲酸甲酯

2-Methoxy-4-Methyl-5-nitro-benzoic acid结构式

2-Methoxy-4-Met...

~%

5-氨基-2-甲氧基-4-甲基苯甲酸甲酯结构式

5-氨基-2-甲氧基-4-甲基苯甲酸甲酯

甲醇结构式

Benzoyl chloride, 4-chloro-2-methoxy-5-nitro结构式

Benzoyl chlorid...

~%

4-氯-2-甲氧基-5-硝基苯甲酸甲酯结构式

4-氯-2-甲氧基-5-硝基苯甲酸甲酯

N-乙基-2-氨甲基吡咯烷结构式

N-乙基-2-氨甲基吡咯烷

~%

N-[(1-ethylpyrrolidin-2-yl)methyl]-5-(methanesulfonamido)-2-methoxy-4-methylbenzamide结构式

N-[(1-ethylpyrr...

2-Methoxy-4-Methyl-5-nitro-benzoic acid结构式

2-Methoxy-4-Met...

~%

N-[(1-ethylpyrrolidin-2-yl)methyl]-5-(methanesulfonamido)-2-methoxy-4-methylbenzamide结构式

N-[(1-ethylpyrr...

甲基磺酰氯结构式

甲基磺酰氯

5-amino-N-((1-ethylpyrrolidin-2-yl)methyl)-2-methoxy-4-methylbenzamide结构式

5-amino-N-((1-e...

~35%

N-[(1-ethylpyrrolidin-2-yl)methyl]-5-(methanesulfonamido)-2-methoxy-4-methylbenzamide结构式

N-[(1-ethylpyrr...

N-((1-ethylpyrrolidin-2-yl)methyl)-2-methoxy-4-methyl-5-nitrobenzamide结构式

N-((1-ethylpyrr...

~%

N-[(1-ethylpyrrolidin-2-yl)methyl]-5-(methanesulfonamido)-2-methoxy-4-methylbenzamide结构式

N-[(1-ethylpyrr...