- Asymmetric Dearomatizing Fluoroamidation of Indole Derivatives with Dianionic Phase-Transfer Catalyst
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Asymmetric dearomatizing fluorocyclization of indole derivatives was investigated using a dicarboxylate phase-transfer catalyst. This reaction proceeds under mild reaction conditions to provide fluoropyrroloindoline derivatives in a highly enantioselective manner. Various substitution patterns on the indole ring are well tolerated. To facilitate the reaction and ensure reproducibility, the addition of water is essential, and its possible role is discussed.
- Egami, Hiromichi,Hotta, Ryo,Otsubo, Minami,Rouno, Taiki,Niwa, Tomoki,Yamashita, Kenji,Hamashima, Yoshitaka
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supporting information
p. 5656 - 5660
(2020/07/14)
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- A substituted indole -3 - acetic acid synthesis method (by machine translation)
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The present invention provides a substituted indole - 3 - acetic acid synthesis method, comprises the following steps: (1) in order to replace the indole as the starting material, with the acylation reagent under the action of catalyst through the tutor - acylation to obtain the 1, 3 - diacetyl substituted indole; (2) intermediate 1, 3 - diacetyl substituted indole does not need refining, directly with the morpholine and sulfur by the Willgerodt - Kindler rearrangement reaction, the inorganic under the catalysis of alkali hydrolysis, acidified to obtain substituted indole - 3 - acetic acid. (by machine translation)
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Paragraph 0067-0069
(2017/05/02)
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- Indole-3-acetic acid derivatives
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Compounds of formula (I), or physiologically functional derivatives thereof, wherein: R1, R2, R3 and R′3 are independently selected from H or lower alkyl; and R4, R5, R6 and R7 are independently selected from H, electron withdrawing groups (such as F, Cl, Br, I, OCF3, carboxyl groups, acetal groups, electron deficient aryl groups), lower alkyl groups, lower alkoxy groups, aryl groups or aryloxy groups, wherein at least one of R4, R5, R6 and R7 is selected from an electron withdrawing group, may be used in methods of therapy, particular in treating neoplastic diseases in methods of GDEPT, ADPET, PDEPT and PDT.
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- Use of indole-3-acetic acid derivatives in medicine
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Compounds of formula (I), or physiologically functional derivatives thereof, wherein: R1, R2, R3 and R′3 are independently selected from II or lower alkyl; and R4, R5, R6 and R7 are independently selected from H, electron withdrawing groups (such as F, Cl, Br, I, OCF3, carboxyl groups, acetal groups, electron deficient aryl groups), lower alkyl groups lower alkoxy groups, aryl groups or aryloxy groups, wherein it least one of R4, R5, R6, and R7 is selected from an electron withdrawing group, may be used in methods of therapy, particular in treating neoplastic diseases in methods of GDEPT, ADPET, PDEPT and PDT
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- USE OF INDOLE-3-ACETIC ACID DERIVATIVES IN MEDICINE
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Compounds of formula (I), or physiologically functional derivatives thereof, wherein: R1, R2, R3 and R'3 are independently selected from II or lower alkyl; and R4, R5, R6 and R7 are independently selected from H, electron withdrawing groups (such as F, Cl, Br, I, OCF3, carboxyl groups, acetal groups, electron deficient aryl groups), lower alkyl groups lower alkoxy groups, aryl groups or aryloxy groups, wherein it least one of R4, R5, R6, and R7 is selected from an electron withdrawing group, may be used in methods of therapy, particular in treating neoplastic diseases in methods of GDEPT, ADPET, PDEPT and PDT
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- Halogenated indole-3-acetic acids as oxidatively activated prodrugs with potential for targeted cancer therapy
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Substituted indole-3-acetic acid (IAA) derivatives, plant auxins with potential for use as prodrugs in enzyme-prodrug directed cancer therapies, were oxidised with horseradish peroxidase (HRP) and toxicity against V79 Chinese hamster lung fibroblasts was determined. Rate constants for oxidation by HRP compound I were also measured. Halogenated IAAs were found to be the most cytotoxic, with typical surviving fractions of -3 after incubation for 2 h with 100 μM prodrug and HRP.
- Rossiter, Sharon,Folkes, Lisa K.,Wardman, Peter
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p. 2523 - 2526
(2007/10/03)
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