Oriental (Luzhou) Agrochemicals Co., Ltd.

Oriental Agrochemicals. Co., Ltd.

Yinwei Sun

Bangchi Chen

Zhongyuan Wang

Pan Zhang

Tao Jin

Teng Lai

Yanyan Huang

Miao Lin

Disclosed are a type of conjugated triene compounds (1), and a preparation and application thereof. In this method, a 2-(cyclohexenylidene)malonic acid derivative is sequentially subjected to isomerization, halogenation reaction in the presence of a halogenating agent and dehydrohalogenation to prepare the conjugated triene compounds (1). This disclosure further provides a method of preparing a 2-aryl malonic acid derivative from the conjugated triene compounds (1) through aromatization reaction.

Conjugated triene compound, and preparation and application thereof

Disclosed herein is a method for preparing a 2-arylmalonic acid derivative. In this method, a cyclohexadiene compound is used as a raw material, and sequentially undergoes an isomerization reaction, a halogenation reaction in the presence of a halogenating agent and a dehydrohalogenation-aromatization reaction to obtain a 2-arylmalonic acid derivative (3). An intermediate for preparing the 2-arylmalonic acid derivative (3) and use of the intermediate are also disclosed.

Method for preparing 2-arylmalonic acid derivative and intermediate, and use thereof

Disclosed are a type of halogenated conjugated diene compounds (1), and preparation and application thereof. In this method, a conjugated diene compounds is subjected to halogenation reaction to prepare the compound (1). This disclosure further provides a method of preparing a 2-arylmalonic acid derivative from the compound (1) through dehydrohalogenation and aromatization reaction. 

Halogenated conjugated diene compound, and preparation and application thereof

Disclosed are a method for preparing 2-(cyclohexenylidene) malonic acid derivatives and uses thereof. In this method, an olefin and a 2-substituted malonic acid derivative are used as starting materials to prepare the 2-(cyclohexenylidene) malonic acid derivative in the presence of a catalyst through cyclization reaction. This method has the following advantages: (1) the method can be very efficiently used for the synthesis of highly sterically-hindered 2-(2,6-disubstituted cyclohexenylidene) malonic acid derivatives; (2) the reaction yield is high, the reaction conditions are mild, and the wastes are less, favorable for industrial production. More importantly, the present invention extends the further use of 2-(cyclohexenylidene)malonic acid derivatives in organic synthesis, especially in the synthesis of 2-aryl malonic acid derivatives and their corresponding drugs such as Pinoxaden.

Method for preparing 2-(cyclohexenylidene) malonic acid derivatives and uses thereof

Disclosed are a method for preparing 2-aryl malonamide and an application thereof. This method uses 2-(cyclohexenylidene) malononitrile as a raw material, which undergoes an aromatization-hydrolyzation reaction in the presence of an oxidant and water to produce 2-aryl malonamide by one step. Compared to the prior art, the method for preparing 2-aryl malonamide of this application has the following features and advantages: (1) this method employs a completely different synthetic strategy; (2) raw materials used in this method are easily obtained; (3) this method not only has high yield, but also does not require expensive metal catalysts. This method is lower-cost, suitable for the industrial production.

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Sichuan, China

Yinwei Sun