92157-09-0Relevant academic research and scientific papers
Novel preparation method of drotaverine hydrochloride intermediate
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, (2019/06/27)
The invention discloses a novel preparation method of a drotaverine hydrochloride intermediate. The preparation method comprises the steps that 1, 4-bromopyrocatechol serves as the raw material and issubjected to an ethylation reaction under the action of iodoethane or diethyl sulfate, and 1,2-diethoxy-4-bromobenzene is prepared; 2, 1,2-diethoxy-4-bromobenzene is subjected to a Suzuki-Miyaura coupling reaction and reacts with ethyl bromoacetate or methyl bromoacetate to prepare 3,4-diethoxyphenylaceticacid ester; 3, 3,4-diethoxyphenylaceticacid is hydrolyzed to prepare 3,4-diethoxyphenylaceticacid; 4, 3,4-diethoxyphenylaceticacid ester and ammonia are prepared into 3,4-diethoxyphenylacetamide; 5, 3,4-diethoxyphenylacetamide is reduced to prepare 3,4-diethoxyphenethylamine. The direct preparation method is used; in the process of preparing 3,4-diethoxyphenyl acetonitrile, application of sodium cyanide is avoided; when 3,4-diethoxyphenethylamine is prepared, lithium aluminium hydride isused for reduction, and a pressurized hydrogenation method is prevented from being used, so that the problems about safety and environment pollution are effectively solved, the process is simple andeasy to implement, and the practicality is high.
New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam
Bihel, Frédéric J.J.,Justiniano, Héléne,Schmitt, Martine,Hellal, Malik,Ibrahim, Mohamed A.,Lugnier, Claire,Bourguignon, Jean-Jacques
scheme or table, p. 6567 - 6572 (2011/12/04)
Pharmacophoric comparison between papaverine and tofisopam led to identify three new series of microto sub-micromolar inhibitors of phosphodiesterase-4, including 7,8-dialkoxy-2,3-benzodiazepin-4-one derivatives, 7,8-dialkoxy-1,4- benzodiazepin-2-one derivatives, and dialkoxybenzophenone derivatives.
