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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 3-(1-substituted-4-piperidinyl)-1, 2-benzisoxazoles

JT Strupczewski, RC Allen, BA Gardner…

文献索引：Strupczewski, Joseph T.; Allen, Richard C.; Gardner, Beth Ann; Schmid, Blaine L.; Stache, Ulrich; et al. Journal of Medicinal Chemistry, 1985 , vol. 28, # 6 p. 761 - 769

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被引用次数: 87

摘要

The synthesis of a series of 34 l-substituted-4-piperidinyl)-1, 2-benzisoxazoles is described. The neuroleptic activity of the series was evaluated by utilizing the climbing mice assay and inhibition of [3H] spiroperidol binding. Structureactivity relationships were studied by variation of the substituent on the benzisoxazole ring with concomitant variation of four different 1-piperidinyl substituents. Maximum neuroleptic activity was realized when there ...

(E)-1-Acetyl-N-(acetyloxy)-α-(5-fluoro-2-hydroxyphenyl)-4-piperidinemethanimine结构式

(E)-1-Acetyl-N-...

~%

3-(1-乙酰基-4-哌啶基)-5-氟-1,2-苯异噁唑结构式

3-(1-乙酰基-4-哌啶基)...

(E)-1-Acetyl-α-(5-fluoro-2-hydroxyphenyl)-N-hydroxy-4-piperidinemethanimine结构式

(E)-1-Acetyl-α-...

~%

3-(1-乙酰基-4-哌啶基)-5-氟-1,2-苯异噁唑结构式

3-(1-乙酰基-4-哌啶基)...

4-哌啶甲酸结构式

甲乙酐结构式

~74%

1-醛基哌啶-4-甲酸结构式

1-醛基哌啶-4-甲酸

乙酸酐结构式

(E)-1-Acetyl-α-(5-fluoro-2-hydroxyphenyl)-N-hydroxy-4-piperidinemethanimine结构式

(E)-1-Acetyl-α-...

~%

(E)-1-Acetyl-N-(acetyloxy)-α-(5-fluoro-2-hydroxyphenyl)-4-piperidinemethanimine结构式

(E)-1-Acetyl-N-...

氯甲酸苄酯结构式

氯甲酸苄酯

2-(5-Methoxy)phenol 4-Piperidinyl Ketone Hydrochloride结构式

2-(5-Methoxy)ph...

~73%

2-(5-Methoxy)phenol 4-(N-Benzyloxycarbonyl)piperidinyl Ketone结构式

2-(5-Methoxy)ph...

4-(N-Acetyl)piperidinyl 2-(5-Methoxy)phenol Ketone结构式

4-(N-Acetyl)pip...

~%

2-(5-Methoxy)phenol 4-(N-Benzyloxycarbonyl)piperidinyl Ketone结构式

2-(5-Methoxy)ph...

N-乙酰基哌啶-4-酰氯结构式

N-乙酰基哌啶-4-酰氯

~%

2-(5-Methoxy)phenol 4-(N-Benzyloxycarbonyl)piperidinyl Ketone结构式

2-(5-Methoxy)ph...

1-乙酰基-4-哌啶甲酸结构式

1-乙酰基-4-哌啶甲酸

~%

2-(5-Methoxy)phenol 4-(N-Benzyloxycarbonyl)piperidinyl Ketone结构式

2-(5-Methoxy)ph...

间苯二甲醚结构式

间苯二甲醚

~%

2-(5-Methoxy)phenol 4-(N-Benzyloxycarbonyl)piperidinyl Ketone结构式

2-(5-Methoxy)ph...

1-醛基哌啶-4-甲酸结构式

1-醛基哌啶-4-甲酸

~%

1-甲酰基-哌啶-4-羰酰氯结构式

1-甲酰基-哌啶-4-羰酰氯

1-乙酰基-4-哌啶甲酸结构式

1-乙酰基-4-哌啶甲酸

~%

1-乙酰基-4-(5-氟-2-羟基苯甲酰基)哌啶结构式

1-乙酰基-4-(5-氟-2-...

4-氟苯甲醚结构式

N-乙酰基哌啶-4-酰氯结构式

N-乙酰基哌啶-4-酰氯

~%

1-乙酰基-4-(5-氟-2-羟基苯甲酰基)哌啶结构式

1-乙酰基-4-(5-氟-2-...

未登录结构式

~%

3-(2-氯乙基)-6,7,8,9-四氢-2-甲基-4H-吡啶并[1,2-a]-嘧啶-4-酮结构式

3-(2-氯乙基)-6,7,8...

1-甲基-4-氯哌啶结构式

1-甲基-4-氯哌啶

~%

3-(2-氯乙基)-6,7,8,9-四氢-2-甲基-4H-吡啶并[1,2-a]-嘧啶-4-酮结构式

3-(2-氯乙基)-6,7,8...

2,6-二氟苯腈结构式

2,6-二氟苯腈

~%

3-(2-氯乙基)-6,7,8,9-四氢-2-甲基-4H-吡啶并[1,2-a]-嘧啶-4-酮结构式

3-(2-氯乙基)-6,7,8...

1-Methyl-4-(2,6-difluorobenzoyl)piperidine结构式

1-Methyl-4-(2,6...

~%

3-(2-氯乙基)-6,7,8,9-四氢-2-甲基-4H-吡啶并[1,2-a]-嘧啶-4-酮结构式

3-(2-氯乙基)-6,7,8...

4-fluoro-3-(1-methyl-4-piperidinyl)-1,2-benzisoxazole结构式

4-fluoro-3-(1-m...

~%

3-(2-氯乙基)-6,7,8,9-四氢-2-甲基-4H-吡啶并[1,2-a]-嘧啶-4-酮结构式

3-(2-氯乙基)-6,7,8...

3-(1-methyl-4-piperidinyl)-1,2-benzisoxazole结构式

3-(1-methyl-4-p...

氯甲酸苯酯结构式

氯甲酸苯酯

~77%

3-(4-Piperidinyl)-1,2-benzisoxazole N-Carbamic Acid Phenyl Ester结构式

3-(4-Piperidiny...

1-甲基-4-氯哌啶结构式

1-甲基-4-氯哌啶

~%

3-(4-Piperidinyl)-1,2-benzisoxazole N-Carbamic Acid Phenyl Ester结构式

3-(4-Piperidiny...

(2-fluorophenyl)-(1-methylpiperidin-4-yl)methanone结构式

(2-fluorophenyl...

~%

3-(4-Piperidinyl)-1,2-benzisoxazole N-Carbamic Acid Phenyl Ester结构式

3-(4-Piperidiny...

2-氟苯甲腈结构式

~%

3-(4-Piperidinyl)-1,2-benzisoxazole N-Carbamic Acid Phenyl Ester结构式

3-(4-Piperidiny...

乙酸酐结构式

(E)-2-(5-Methoxy)phenol 4-(N-Benzyloxycarbonyl)piperidinyl-methanone Oxime结构式

(E)-2-(5-Methox...

~%

(E)-2-(5-Methoxy)phenol 4-(N-Benzyloxycarbonyl)piperidinyl-methanone O-Acetyl Oxime结构式

(E)-2-(5-Methox...

4-(N-Acetyl)piperidinyl 2-(5-Methoxy)phenol Ketone结构式

4-(N-Acetyl)pip...

~70%

2-(5-Methoxy)phenol 4-Piperidinyl Ketone Hydrochloride结构式

2-(5-Methoxy)ph...

1-乙酰基-4-哌啶甲酸结构式

1-乙酰基-4-哌啶甲酸

~%

2-(5-Methoxy)phenol 4-Piperidinyl Ketone Hydrochloride结构式

2-(5-Methoxy)ph...

N-乙酰基哌啶-4-酰氯结构式

N-乙酰基哌啶-4-酰氯

~%

2-(5-Methoxy)phenol 4-Piperidinyl Ketone Hydrochloride结构式

2-(5-Methoxy)ph...

间苯二甲醚结构式

间苯二甲醚

~%

2-(5-Methoxy)phenol 4-Piperidinyl Ketone Hydrochloride结构式

2-(5-Methoxy)ph...

1-乙酰基-4-哌啶甲酸结构式

1-乙酰基-4-哌啶甲酸

~%

4-(N-Acetyl)piperidinyl 2-(5-Methoxy)phenol Ketone结构式

4-(N-Acetyl)pip...

N-乙酰基哌啶-4-酰氯结构式

N-乙酰基哌啶-4-酰氯

间苯二甲醚结构式

间苯二甲醚

~%

4-(N-Acetyl)piperidinyl 2-(5-Methoxy)phenol Ketone结构式

4-(N-Acetyl)pip...