955892-12-3Relevant articles and documents
Synthetic method of tert-butyl-7-hydroxy-7,8-dihydro-4H-pyrazolo [1,5-a][1,4] diazepin-5-(6H)-carboxylate
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Paragraph 0007, (2017/10/22)
The invention relates to a synthetic method of tert-butyl-7-hydroxy-7,8-dihydro-4H-pyrazolo [1,5-a][1,4] diazepin-5-(6H)-carboxylate and mainly solves the technical problems of low perfect ratio of a route, difficulty in reaction control, inconvenience in experiment operation and the like in the conventional synthetic process. Tert-butyl-7-hydroxy-7,8-dihydro-4H-pyrazolo [1,5-a][1,4] diazepin-5-(6H)-carboxylate is prepared from 1,1-dimethoxypropane-2-one serving as a starting material through six steps of reactions. The equation is shown in the specification. The obtained product diazepine is a useful intermediate or product for synthesis of various drugs.
Highly active binuclear Cu(II) catalyst bearing an unsymmetrical bipyridine-pyrazole-amine ligand for the azide-alkyne cycloaddition reaction
Han, Baofeng,Xiao, Xiao,Wang, Lan,Ye, Wenjing,Liu, Xiaoping
, p. 1446 - 1450 (2016/10/04)
Ligands containing NH groups often show special characteristics. In this paper, a well-defined dinuclear Cu(II) complex bearing an unsymmetrical bipyridine-pyrazole-amine ligand was synthesized by the condensation of N–H to release H2O. Using sodium L-ascorbate as a reductant, the binuclear complex showed excellent activity in 1,3-dipolar cycloaddition reactions between alkynes and azides to obtain 1,4-disubstituted triazoles in 95%–99% isolated yields.
Bu3SnH-mediated radical cyclisation onto azoles
Allin, Steven M.,Barton, William R.S.,Russell Bowman,Bridge (née Mann), Emma,Elsegood, Mark R.J.,McInally, Tom,McKee, Vickie
, p. 7745 - 7758 (2008/12/21)
Alkyl radicals have been cyclised onto pyrroles, imidazoles and pyrazoles, and acyl radicals cyclised onto pyrroles, using Bu3SnH-, (TMS)3SiH- and Bu3GeH-mediated aromatic homolytic substitution for the synthesis of bicyclic N-heterocycles. The reactions yield intermediate π-radicals that lose hydrogen in the?rearomatisation step of the aromatic homolytic substitution. Mechanistic studies of these rearomatisation steps indicate aromatic homolytic substitution in which the initiator or breakdown products from the inhibitor are responsible for the H-abstraction step.
Indium(III)trifluoromethanesulfonate as a mild, efficient catalyst for the formation of acetals and ketals in the presence of acid sensitive functional groups
Gregg, Brian T.,Golden, Kathryn C.,Quinn, John F.
, p. 3287 - 3295 (2008/09/21)
Aldehydes and ketones, including acetophenone and benzophenone, are readily protected under mild, neutral conditions in the presence of various alcohols or orthoformates and catalytic amounts of indium(III) trifluoromethanesulfonate (0.8 mol %) under either room temperature or mild heating conditions to give the corresponding cyclic and acyclic acetals and ketals in good to excellent yields. Acid sensitive functional groups, N-Boc, THP, and TBDMS do not undergo competitive deprotection under the reported conditions.
Synthesis and biological activities of meribendan and related heterocyclic benzimidazolo-pyridazinones
Jonas, R,Klockow, M,Lues, I,Pruecher, H,Schliep, H J,Wurziger, H
, p. 129 - 140 (2007/10/02)
The synthesis of a new heterocyclic benzimidazolo-pyridazinones is described.The new compounds were evaluated as inotropic agents with 'calcium-sensitizing' effects. 5-Methyl-6--2,3,4,5-tetrahydro-pyridazin-3-one hydrochloride (meribendan) turned out to be the most interesting compound and was chosen for development as a positive inotrope. benzimidazole / calcium sensivity / cardiotonics / inotropes / phosphodiesterase / papillary muscle / pyridazinone