- Sassafras oil, carrot bits and microwaves: Green lessons learned from the formal total synthesis of (-)-talampanel
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A formal total synthesis of (-)-talampanel (1), a 2,3-benzodiazepine is described. This work was undertaken to utilize greener reaction conditions. Safrole (a renewable source) was converted to (1) in eight steps, including an enantioselective bioreduction using carrots as the key step. Microwave irradiation was also used to perform three reaction steps.
- Omori, Alvaro Takeo,De Oliveira, Camila De Souza,Andrade, Kleber Tellini,Capeletto, Marina Gon?alves
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p. 103563 - 103565
(2015/12/23)
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- Crystalline form of dihydro-2,3-benzodiazepine derivative
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A physical form of (R)-7-acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine having an X-ray powder diffraction pattern with d spacings at 12.78, 9.48, 8.99, 8.64, 8.23, 6.39, 6.27. 5.73, 4.01 and 3.96 ?. The compound is
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- Physical form of dihydro-2,3-benzodiazepine derivative
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A physical form of (R)-7-acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine having an X-ray powder diffraction pattern with d spacings at 10.61, 8.83, 6.78, 5.83, 4.13 and 3.74 ?. The compound is useful as an AMPA antag
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- Synthesis and anticonvulsant activity of 3-aryl-5H-2,3-benzodiazepine AMPA antagonists
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A novel series of 3-aryl-5H-2,3-benzodiazepines with N-3 aromatic substituents has been synthesized. Good in vivo anticonvulsant activity of the new compounds has been demonstrated employing the maximal electroshock seizure test in mice. Evaluation of a subset of the compounds in the cortical wedge assay confirmed the new structures to be AMPA antagonists.
- Anderson, Benjamin A.,Harn, Nancy K.,Hansen, Marvin M.,Harkness, Allen R.,Lodge, David,Leander, J. David
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p. 1953 - 1956
(2007/10/03)
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- STEREOSELECTIVE PROCESS FOR PRODUCING DIHYDRO-2,3-BENZODIAZEPINE DERIVATIVES
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A process for stereoselectively forming N-substituted dihydro-2,3 benzodiazepines which are useful as AMPA receptor antagonists. The process includes an opening reduction step which sets the stereochemistry of the intermediates and the final compounds to
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