The Experts below are selected from a list of 294 Experts worldwide ranked by ideXlab platform
Philippe Belmont - One of the best experts on this subject based on the ideXlab platform.
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visible light amination smiles cascade access to Phthalazine derivatives
Chemical Science, 2016Co-Authors: Etienne Brachet, Leyre Marzo, Mohamed Selkti, Burkhard Konig, Philippe BelmontAbstract:We report the synthesis of various Phthalazines via a new cascade reaction, initiated by visible light photocatalysis, involving a radical hydroamination reaction followed by a radical Smiles rearrangement. Phthalazine derivatives are obtained in high yields and from a broad scope readily accessible ortho-alkynylsulfonohydrazone precursors. The mild photoredox conditions ensure an excellent functional group tolerance. Application of this strategy to a one-pot protocol starting from the corresponding carbonyl compounds, and subsequent functionalization allow the rapid synthesis of structurally diverse structures.
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Visible light amination/Smiles cascade: access to Phthalazine derivatives.
Chemical Science, 2016Co-Authors: Etienne Brachet, Leyre Marzo, Mohamed Selkti, Burkhard Konig, Philippe BelmontAbstract:We report the synthesis of various Phthalazines via a new cascade reaction, initiated by visible light photocatalysis, involving a radical hydroamination reaction followed by a radical Smiles rearrangement. Phthalazine derivatives are obtained in high yields and from a broad scope readily accessible ortho-alkynylsulfonohydrazone precursors. The mild photoredox conditions ensure an excellent functional group tolerance. Application of this strategy to a one-pot protocol starting from the corresponding carbonyl compounds, and subsequent functionalization allow the rapid synthesis of structurally diverse structures.
Etienne Brachet - One of the best experts on this subject based on the ideXlab platform.
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visible light amination smiles cascade access to Phthalazine derivatives
Chemical Science, 2016Co-Authors: Etienne Brachet, Leyre Marzo, Mohamed Selkti, Burkhard Konig, Philippe BelmontAbstract:We report the synthesis of various Phthalazines via a new cascade reaction, initiated by visible light photocatalysis, involving a radical hydroamination reaction followed by a radical Smiles rearrangement. Phthalazine derivatives are obtained in high yields and from a broad scope readily accessible ortho-alkynylsulfonohydrazone precursors. The mild photoredox conditions ensure an excellent functional group tolerance. Application of this strategy to a one-pot protocol starting from the corresponding carbonyl compounds, and subsequent functionalization allow the rapid synthesis of structurally diverse structures.
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Visible light amination/Smiles cascade: access to Phthalazine derivatives.
Chemical Science, 2016Co-Authors: Etienne Brachet, Leyre Marzo, Mohamed Selkti, Burkhard Konig, Philippe BelmontAbstract:We report the synthesis of various Phthalazines via a new cascade reaction, initiated by visible light photocatalysis, involving a radical hydroamination reaction followed by a radical Smiles rearrangement. Phthalazine derivatives are obtained in high yields and from a broad scope readily accessible ortho-alkynylsulfonohydrazone precursors. The mild photoredox conditions ensure an excellent functional group tolerance. Application of this strategy to a one-pot protocol starting from the corresponding carbonyl compounds, and subsequent functionalization allow the rapid synthesis of structurally diverse structures.
Zhe-shan Quan - One of the best experts on this subject based on the ideXlab platform.
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synthesis and primary anticonvulsant activity evaluation of 6 alkyoxyl tetrazolo 5 1 a Phthalazine derivatives
Drug Research, 2011Co-Authors: Xianqing Deng, Zhe-shan QuanAbstract:A new series of 6-alkyoxyl-tetrazolo[5,l- a ] Phthalazine derivatives (4 a-4 o) were synthesized as potential anticonvulsant agents. Anticonvulsant activity was evaluated by the maximal electroshock (MES) test. Neurotoxicity was evaluated by the rotarod neurotoxicity test. The pharmacological results showed that 6-(4-chlorophenyoxyl) - tetrazolo [5,1- a ] Phthalazine (4 m) was the most potent agent, with a median effective dose (ED 50 ) of 6.8 mg/kg and a median neurotoxic dose (TD 50 ) of 456.4 mg/kg. The protective index (PI = TD50/ED50) for compound 4 m was 67.1, which was significantly higher than that for the reference drug carbamazepine (PI = 6.4).
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synthesis and anti inflammatory activity evaluation of some novel 6 alkoxy phenoxy 1 2 4 triazolo 3 4 a Phthalazine 3 amine derivatives
European Journal of Medicinal Chemistry, 2010Co-Authors: Chuan Hu, Xianqing Deng, Zhe-shan QuanAbstract:Abstract Starting from phthalic anhydride, several new 6-alkoxy(phenoxy)-[1,2,4]triazolo[3,4- a ]Phthalazine-3-amine derivatives were synthesized as potent anti-inflammatory agent. The study showed that the compounds 6h (6-(2-chlorophenoxy)-[1,2,4]triazolo[3,4- a ]Phthalazine-3-amine) and 6s (6-(4-aminophenoxy)-[1,2,4] triazolo[3,4- a ]Phthalazine-3-amine) exhibited the highest anti-inflammatory activity (81% and 83% inhibition, respectively, at 0.5 h after i.p. administration) which were slightly more potent than the reference drug Ibuprofen (61%). Furthermore, the peak activity of 6h and 6s was observed at the 3 h after p.o. administration, and they exhibited stronger anti-inflammatory activity than Ibuprofen at the dose of 50 mg/kg at the peak time.
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Synthesis and anticonvulsant activity of 6-alkoxy-[1,2,4]triazolo[3,4-a]Phthalazines.
Chemical Biology & Drug Design, 2009Co-Authors: Lei Zhang, Li-ping Guan, Kyu-yun Chai, Zhe-shan QuanAbstract:: A new series of 6-alkoxy-[1,2,4]triazolo[3,4-a]Phthalazines (3a-3v) were synthesized and their anticonvulsant activity and neurotoxicity were evaluated by the maximal electroshock test and the rotarod test respectively. Significant anticonvulsant activity was displayed by a number of compounds. The most promising compounds 6-(4-chlorobenzyloxy)-[1,2,4]triazolo[3,4-a]Phthalazine (3f) and 6-heptyloxy-[1,2,4]triazolo[3,4-a]Phthalazine (3s) showed a median effective dose of 7.1 and 11.0 mg/kg, and had protective index value of 5.2 and 8.0 respectively. The two compounds were further found to have potent activity against seizures induced by pentylenetetrazole, isoniazid, thiosemicarbazide, 3-mercaptopropionic acid but not seizures induced by strychnine, indicating that the two compounds might function by enhancing gamma-aminobutyric acid neurotransmission.
Mohamed Selkti - One of the best experts on this subject based on the ideXlab platform.
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visible light amination smiles cascade access to Phthalazine derivatives
Chemical Science, 2016Co-Authors: Etienne Brachet, Leyre Marzo, Mohamed Selkti, Burkhard Konig, Philippe BelmontAbstract:We report the synthesis of various Phthalazines via a new cascade reaction, initiated by visible light photocatalysis, involving a radical hydroamination reaction followed by a radical Smiles rearrangement. Phthalazine derivatives are obtained in high yields and from a broad scope readily accessible ortho-alkynylsulfonohydrazone precursors. The mild photoredox conditions ensure an excellent functional group tolerance. Application of this strategy to a one-pot protocol starting from the corresponding carbonyl compounds, and subsequent functionalization allow the rapid synthesis of structurally diverse structures.
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Visible light amination/Smiles cascade: access to Phthalazine derivatives.
Chemical Science, 2016Co-Authors: Etienne Brachet, Leyre Marzo, Mohamed Selkti, Burkhard Konig, Philippe BelmontAbstract:We report the synthesis of various Phthalazines via a new cascade reaction, initiated by visible light photocatalysis, involving a radical hydroamination reaction followed by a radical Smiles rearrangement. Phthalazine derivatives are obtained in high yields and from a broad scope readily accessible ortho-alkynylsulfonohydrazone precursors. The mild photoredox conditions ensure an excellent functional group tolerance. Application of this strategy to a one-pot protocol starting from the corresponding carbonyl compounds, and subsequent functionalization allow the rapid synthesis of structurally diverse structures.
Leyre Marzo - One of the best experts on this subject based on the ideXlab platform.
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visible light amination smiles cascade access to Phthalazine derivatives
Chemical Science, 2016Co-Authors: Etienne Brachet, Leyre Marzo, Mohamed Selkti, Burkhard Konig, Philippe BelmontAbstract:We report the synthesis of various Phthalazines via a new cascade reaction, initiated by visible light photocatalysis, involving a radical hydroamination reaction followed by a radical Smiles rearrangement. Phthalazine derivatives are obtained in high yields and from a broad scope readily accessible ortho-alkynylsulfonohydrazone precursors. The mild photoredox conditions ensure an excellent functional group tolerance. Application of this strategy to a one-pot protocol starting from the corresponding carbonyl compounds, and subsequent functionalization allow the rapid synthesis of structurally diverse structures.
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Visible light amination/Smiles cascade: access to Phthalazine derivatives.
Chemical Science, 2016Co-Authors: Etienne Brachet, Leyre Marzo, Mohamed Selkti, Burkhard Konig, Philippe BelmontAbstract:We report the synthesis of various Phthalazines via a new cascade reaction, initiated by visible light photocatalysis, involving a radical hydroamination reaction followed by a radical Smiles rearrangement. Phthalazine derivatives are obtained in high yields and from a broad scope readily accessible ortho-alkynylsulfonohydrazone precursors. The mild photoredox conditions ensure an excellent functional group tolerance. Application of this strategy to a one-pot protocol starting from the corresponding carbonyl compounds, and subsequent functionalization allow the rapid synthesis of structurally diverse structures.
