79101-83-0Relevant articles and documents
PROCESS FOR THE PREPARATION OF CHLORANTRANILIPROLE
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, (2021/02/26)
The present invention relates to two novel, efficient and one-pot methods for synthesizing chlorantraniliprole. In the first scheme, Chlorantraniliprole is prepared by a novel telescopic process starting from 3-Bromo-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-carboxylic acid a key raw material-A (Key RM-A). In the second scheme, starting from Key RM-A, the process steps use of a novel variant of anthranilic acid (Methyl 2-amino-5-chloro-3-methylbenzoate), to get Chlorantraniliprole. Furthermore, the present invention also relates to the synthesis of key starting material for the synthesizing chlorantraniliprole in-situ. All the in-situ steps of the disclosed synthesis methods obtain good yield, without using any expensive reagent or base or harsh reaction conditions, which makes the process simple, environment friendly and more cost effective. With this process the production cost of chlorantraniliprole and its intermediates is substantially reduced; fewer by-products are formed during its synthesis and since it's a one-pot reaction, isolation and purification are easy to achieve.
2-amino-5-chloro-N,3-dimethylbenzamide preparation method
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, (2020/03/09)
The invention discloses a 2-amino-5-chloro-N,3-dimethylbenzamide preparation method, which comprises: carrying out a chlorination reaction a raw material represented by a formula I and a chlorinationreagent at the ortho-position and the para-position of amino to generate a compound represented by a formula II, carrying out a selective substitution reaction on the compound represented by the formula II and a cyano group mainly based on amino o-chlorine substitution under an alkaline catalysis condition by utilizing the thermodynamic stability difference between the o-chlorine and the p-chlorine of amino to generate a compound represented by a formula III, hydrolyzing the compound represented by the formula III into a compound represented by a formula IV, esterifying the compound represented by the formula IV to generate a compound represented by a formula V, and carrying out a reaction on the compound represented by the formula V and a monomethylamine methanol solution to generate 2-amino-5-chloro-N,3-dimethylbenzamide. According to the invention, the preparation method is high in yield, simple in reaction and small in toxic and side effects.
Asymmetric Synthesis of Fused Polycyclic Indazoles through Aminocatalyzed Aza-Michael Addition/Intramolecular Cyclization
Giardinetti, Maxime,Marrot, Jér?me,Moreau, Xavier,Coeffard, Vincent,Greck, Christine
, p. 6855 - 6861 (2016/08/16)
The first example of an asymmetric aminocatalyzed aza-Michael addition of 1H-indazole derivatives to α,β-unsaturated aldehydes is described. The iminium/enamine cascade process lies at the heart of our strategy, leading to enantioenriched fused polycyclic indazole architectures. Variations on both the α,β-unsaturated aldehydes and the indazole-7-carbaldehyde heterocycles were studied in order to broaden the scope of the transformation in synthetically interesting directions. The fused polycyclic indazoles exhibit fluorescence properties and can undergo synthetic transformations.