scholarly journals β-Nitroacrylates: New Key Precursors of Indole-2-Carboxylates via Fischer Indole Synthesis

2019 ◽  
Vol 9 (23) ◽  
pp. 5168 ◽  
Author(s):  
Gabrielli ◽  
Panmand ◽  
Ballini ◽  
Palmieri
Keyword(s):  
Point Of View ◽  
Biologically Active ◽  
Fischer Indole Synthesis ◽  
Work Up ◽  
Indole Synthesis

Indole 2-carboxylates are very important scaffolds that are widely investigated for their activities and are used as key intermediates of biologically active molecules. Herein, we report a new procedure for the preparation of this class of derivatives, via Fischer indole synthesis, starting from β-nitroacrylates and arylhydrazines. The protocol permits the production of the title targets in satisfactory overall yields, avoids any wasteful aqueous work-up, and has with evident advantages from a sustainability point of view.

SO3H-Functionalized Ionic Liquids-Catalyzed Facile and Efficient Procedure for Fischer Indole Synthesis under Ultrasound Irradiation

2013 ◽  
Vol 661 ◽  
pp. 150-153 ◽  
Author(s):  
Li Li Tao ◽  
Jing Jiang ◽  
Ye Chu Pan ◽  
Xin Yang ◽  
Bai Lin Li
Keyword(s):  
Ionic Liquids ◽  
Reaction Times ◽  
Environmentally Friendly ◽  
Ultrasound Irradiation ◽  
Practical Method ◽  
Efficient Synthesis ◽  
Efficient Procedure ◽  
Fischer Indole Synthesis ◽  
Work Up ◽  
Indole Synthesis

A facile and efficient synthesis of indole has been developed using ketones or cyclohexandiones with aryhydrazine hydrochlorides in 85% to 95% yields in water under ultrasound irradiation in the presence of Novel SO3H-functionalized ionic liquids (ILs) catalyst. Simple work-up procedure, environmentally friendly, inexpensive and non-toxic catalyst, shorter reaction times along with excellent product yields are the significant features of this practical method.

scholarly journals Fischer indole synthesis applied to the total synthesis of natural products

RSC Advances ◽  
2017 ◽  
Vol 7 (83) ◽  
pp. 52852-52887 ◽  
Author(s):  
Majid M. Heravi ◽  
Sahar Rohani ◽  
Vahideh Zadsirjan ◽  
Nazli Zahedi
Keyword(s):  
Natural Products ◽  
Total Synthesis ◽  
Biologically Active ◽  
Crucial Step ◽  
Fischer Indole Synthesis ◽  
Indole Synthesis ◽  
Active Natural

In this review, we are trying to underscore the application of FIS in one of the crucial step of indole construction in the total synthesis of biologically active natural products.

Analogues of the cholecystokinin octapeptide modified in the central part of the molecule

1991 ◽  
Vol 56 (9) ◽  
pp. 1963-1970 ◽  
Author(s):  
Jan Hlaváček ◽  
Václav Čeřovský ◽  
Jana Pírková ◽  
Pavel Majer ◽  
Lenka Maletínská ◽  
...  
Keyword(s):  
Amino Acid ◽  
Biological Activities ◽  
Point Of View ◽  
Biologically Active ◽  
Side Chain ◽  
Amino Acid Residues ◽  
Cholecystokinin Octapeptide ◽  
Biological Tests ◽  
Biological Potency ◽  
Biologically Active Conformation

In a series of analogues of the cholecystokinin octapeptide (CCK-8) the amino acid residues were gradually modified by substituting Gly by Pro in position 4, Trp by His in position 5, Met by Cle in position 6, or the Gly residue was inserted between Tyr and Met in positions 2 and 3 of the peptide chain, and in the case of the cholecystokinin heptapeptide (CCK-7) the Met residues were substituted by Nle or Aib. These peptides were investigated from the point of view of their biological potency in the peripheral and central region. From the results of the biological tests it follows that the modifications carried out in these analogues and in their Nα-Boc derivatives mean a suppression of the investigated biological activities by 2-3 orders of magnitude (at a maximum dose of the tested substance of 2 . 10-2 mg per animal).This means that a disturbance of the assumed biologically active conformation of CCK-8, connected with a considerable decrease of the biological potency of the molecule, takes place not only after introduction of the side chain into its centre (substitution of Gly4), but also after the modification of the side chains of the amino acids or by extension of the backbone in further positions around this central amino acid.

Modular Counter-Fischer–Indole Synthesis through Radical-Enolate Coupling

2021 ◽  
Vol 23 (3) ◽  
pp. 1096-1102
Author(s):  
Hyunho Chung ◽  
Jeongyun Kim ◽  
Gisela A. González-Montiel ◽  
Paul Ha-Yeon Cheong ◽  
Hong Geun Lee
Keyword(s):  
Fischer Indole Synthesis ◽  
Indole Synthesis

A continuous flow microwave-assisted fischer indole synthesis of 7-Ethyltryptophol

2017 ◽  
Vol 121 ◽  
pp. 144-148 ◽  
Author(s):  
Jianguo Xu ◽  
Jiangang Yu ◽  
Yi Jin ◽  
Jie Li ◽  
Zhiqun Yu ◽  
...  
Keyword(s):  
Continuous Flow ◽  
Microwave Assisted ◽  
Fischer Indole Synthesis ◽  
Indole Synthesis

scholarly journals Bariatric Surgery in Adults: Patient Workup and Preparation

2020 ◽  
pp. 8-14
Author(s):  
Ravi Kant ◽  
Shankar Roy ◽  
Pradeep Yadav KL ◽  
Monika Pathania
Keyword(s):  
Risk Factors ◽  
Metabolic Disease ◽  
Bariatric Surgery ◽  
Metabolic Syndrome ◽  
Morbid Obesity ◽  
Life Style ◽  
Point Of View ◽  
Related Complication ◽  
Initial Intervention ◽  
Work Up

With the advancement and industrialization of our society, the prevalence of metabolic disease is also increasing. Among the risk factors for metabolic syndrome and many other non-communicable diseases, obesity is the single most important one. Although life style and pharmacological therapies are the part of initial intervention, however once the overt obesity related complication appears, bariatric surgery becomes the only curative intervention. Various modalities surgeries have come into place in recent times. However preparing a patient physically and mentally needs a thorough pre- operative preparation. Here in this review, we are exploring the approach to patient with morbid obesity and work up for bariatric surgery from a physician’s point of view.

scholarly journals Polyphosphate Ester as a Synthetic Agent. V. The Fischer Indole Synthesis with Polyphosphate Ester

1966 ◽  
Vol 14 (9) ◽  
pp. 934-939 ◽  
Author(s):  
Yuichi Kanaoka ◽  
Yoshio Ban ◽  
Koichi Miyashita ◽  
Kimiko Irie ◽  
Osamu Yonemitsu
Keyword(s):  
Fischer Indole Synthesis ◽  
Indole Synthesis
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