<b>1-(Indolylalkyl)-4-Arylpiperazines: A New Class of Tranquilizers</b>

Archer, Sydney; Wylie, David W.; Harris, L. S.; Lewis, Thomas R.; Schulenberg, John W.; Bell, Malcolm R.; Kullnig, Rudolph K.; P, Arnold A

doi:10.1021/ja00866a050

Cited by 35 publications

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“…When the alcohols was replaced by amines, the corresponding urea derivatives 31-33 were obtained. It is noteworthy that when the acid azide 24 was heated in an excess of hydrazine hydrate, Curtius rearrangement did not occur and the product was [1,3,4] thiadiazine 34. Whereas, its reaction with chloro acetone did not give the thiadiazine 36 but gave the corresponding acetonylthio derivative 35.…”

Section: Resultsmentioning

confidence: 99%

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Synthesis, Reactions and Antimicrobial Activity of Some New Indolyl‐1,3,4‐Oxadiazole, Triazole and Pyrazole Derivatives

Abdel-Rahman

Farghaly

2004

J Chinese Chemical Soc

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Indole‐3‐carboxylic acid hydrazide 3 was prepared and was treated with aromatic aldehydes in ethanol to give the corresponding hydrazone derivatives 4–7 in good yields. The indole carbohydrazide was incorporated into the 3‐indolyloxadiazoles 8–11 and 18, 3‐indolyltriazoles 13–17 and 35, 3‐indolylpyrazole derivatives 19–23 and carbamate derivatives 26–27. Furthermore, interaction of the carboazide 24 with hydrazine hydrate in refluxing toluene afforded the corresponding semicarbazide derivative 30. The thiadiazine derivative 34 was also prepared. Some of these compounds were screened in vitro for their antibacterial and antifungal activity.

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Section: Resultsmentioning

confidence: 99%

“…1,2 Several of these derivatives possess potent central nervous system (CNS) as well as anti-inflammatory properties. [3][4][5][6] Indole-3carbohydrazide derivatives have been shown to inhibit monoamine oxidase A activity. 7-9 Some N-methylindol-3hydrazones have shown antihypertensive activity in spontaneously hypertensive rates.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Reactions and Antimicrobial Activity of Some New Indolyl‐1,3,4‐Oxadiazole, Triazole and Pyrazole Derivatives

Abdel-Rahman

Farghaly

2004

J Chinese Chemical Soc

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“…[26] Thel atter is prepared by oxone-mediated oxidation of 9 and methylation. Theindole core of the antipsychotic oxypertine (24) [27] can be completed by methylation and debenzylation of 1l,h ighlighting an efficient and chemoselective dissolving metal reduction of the N-Bn group that does not reduce the indole. Finally,polyfunctional indoloquinone 25 was prepared by C7 borylation/oxidation.…”

Section: Methodsmentioning

confidence: 99%

A Bioinspired Synthesis of Polyfunctional Indoles

et al. 2018

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Polyfunctional indoles bearing substituents at C5 and C6 are prevalent in natural products, pharmaceuticals, agrochemicals, and materials. Owing to the remoteness of the C5 and C6 positions, indoles of this family can be difficult to prepare, and often require multistep syntheses. Herein, we describe a concise process that converts simple derivatives of tyrosine into 5,6-difunctionalized indoles by direct oxidation of C-H, N-H, and O-H bonds. Our work draws inspiration from the biosynthetic polymerization of tyrosine to make melanin pigments, but makes an important departure to provide well-defined indole heterocycles.

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“…The latter is prepared by oxone‐mediated oxidation of 9 and methylation. The indole core of the antipsychotic oxypertine ( 24 ) can be completed by methylation and debenzylation of 1 l , highlighting an efficient and chemoselective dissolving metal reduction of the N ‐Bn group that does not reduce the indole. Finally, polyfunctional indoloquinone 25 was prepared by C7 borylation/oxidation.…”

Section: Methodsmentioning

confidence: 99%

A Bioinspired Synthesis of Polyfunctional Indoles

et al. 2018

View full text Add to dashboard Cite

Polyfunctional indoles bearing substituents at C5 and C6 are prevalent in natural products, pharmaceuticals, agrochemicals, and materials. Owing to the remoteness of the C5 and C6 positions, indoles of this family can be difficult to prepare, and often require multistep syntheses. Herein, we describe a concise process that converts simple derivatives of tyrosine into 5,6‐difunctionalized indoles by direct oxidation of C−H, N−H, and O−H bonds. Our work draws inspiration from the biosynthetic polymerization of tyrosine to make melanin pigments, but makes an important departure to provide well‐defined indole heterocycles.

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1-(Indolylalkyl)-4-Arylpiperazines: A New Class of Tranquilizers

Cited by 35 publications

References 0 publications

Synthesis, Reactions and Antimicrobial Activity of Some New Indolyl‐1,3,4‐Oxadiazole, Triazole and Pyrazole Derivatives

Synthesis, Reactions and Antimicrobial Activity of Some New Indolyl‐1,3,4‐Oxadiazole, Triazole and Pyrazole Derivatives

A Bioinspired Synthesis of Polyfunctional Indoles

A Bioinspired Synthesis of Polyfunctional Indoles

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