| 摘要 |
PURPOSE:The one-pot process for the production of the titled compound which is used as an intermediate of penicillin, antipimelotic and antifermentative can be done by reaction between a hydrazine and acrylonitrile, followed by addition of an aqueous solution of mineral acid to the reaction adduct. CONSTITUTION:A compound of formula I (R is H, lower alkyl) is allowed to react with acrylonitrile to form an adduct of formula II, which is combined with a minieral acid such as hydrochloric, sulfuric or phosphoric acid, preferably aqueous hydrochloric or sulfuric acid, to effect the reaction, preferably at the refluxing temperature to produce the objective compound of formula III through one-pot process in no need of separation of intermediate products. Further, the process according to the present invention can minimize the amount of mineral acid required in the process, further ethanol is unnecessary. The process has following additional advantages: freeness from violent heat libration, dangerous precipitation of a large amount of crystals and filtration operation requiring hours.
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