Abstract: Disclosed herein are a preparation method and an application of an isoxazinone compound (I), where the preparation method includes: reacting compound (II) with a carboxylic acid (III) in the presence of a dehydrating agent and a base to produce the isoxazinone compound (I); and subjecting the isoxazinone compound (I) and a protonic acid salt of an amino compound (IV) or R3OH (VII) to ring-opening reaction in the presence of a base to produce a bisamide compound (V) or an N-acyl benzoate compound (VI).

Abstract: The application provides a high-purity thermostable crystal form of a substituted 3-isoxazolidinone compound, a preparation method therefor and an application thereof. The High-purity thermostable crystal form is prepared by a particular method of the present technology and is determined by single-crystal X-ray diffraction as an orthorhombic crystal, featuring a space group of P212121 and lattice parameters of a=9.2301(2) ?, b=11.0751(3) ?, c=12.7554(3) A, ?=90°, ?=90°, and ?=90°. The orthorhombic crystal can be conveniently applied in preparation of agrochemical formulations, such as a suspension concentrate and a water dispersible granule, and the new formulations prepared have a better herbicidal activity and crop safety.

Abstract: Disclosed herein is a method of preparing N-acyl anthranilamide (I), including: reacting a substituted anthranilic acid (II) with pyrazolecarboxylic acid (III) under the action of a phosphorus reagent and a base to obtain an intermediate benzoxazinone (IV); and subjecting the intermediate benzoxazinone (IV) and a protonic acid salt of methylamine to a ring-opening reaction to obtain N-acyl anthranilamide (I), as shown in the following reaction scheme: where X is hydrogen, chloro or cyano group; and HY is hydrohalic acid, sulfuric acid, phosphoric acid or a carboxylic acid. The method has the advantages of simple operation, mild reaction conditions, less waste and high overall yield, and thus is suitable for industrial production.

Abstract: Disclosed is a method of synthesizing 1,2,4-triazole-3-thione compounds and intermediates thereof. The method includes reacting a hydrazine with glyoxylic acid to form a hydrazono acetic acid intermediate followed by reacting the latter with thiocyanate to obtain the 1,2,4-triazole-3-thione compound. The raw materials involved in the present method are readily available, and the reaction is very specific in terms of regioselectivity, resulting in minimum by-product and high product yield. There are neither specific requirements for special equipment nor special operations such as high vacuum, high temperature, anhydrous and oxygen-free manipulations. The process is simple and generates minimum wastes, suitable for industrial production.

Abstract: Disclosed herein are a preparation method and an application of an isoxazinone compound (I), where the preparation method includes: reacting compound (II) with a carboxylic acid (III) in the presence of a dehydrating agent and a base to produce the isoxazinone compound (I); and subjecting the isoxazinone compound (I) and a protonic acid salt of an amino compound (IV) or R3OH (VII) to ring-opening reaction in the presence of a base to produce a bisamide compound (V) or an N-acyl benzoate compound (VI).

Abstract: Disclosed herein is a method of preparing N-acyl anthranilamide (I), including: reacting a substituted anthranilic acid (II) with pyrazolecarboxylic acid (III) under the action of a phosphorus reagent and a base to obtain an intermediate benzoxazinone (IV); and subjecting the intermediate benzoxazinone (IV) and a protonic acid salt of methylamine to a ring-opening reaction to obtain N-acyl anthranilamide (I), as shown in the following reaction scheme: where X is hydrogen, chloro or cyano group; and HY is hydrohalic acid, sulfuric acid, phosphoric acid or a carboxylic acid. The method has the advantages of simple operation, mild reaction conditions, less waste and high overall yield, and thus is suitable for industrial production.

Abstract: Disclosed are a method of synthesizing prothioconazole and optically active isomers thereof and intermediates. The method includes reacting hydrazine with glyoxylic acid to produce a hydrazono acetic acid as an intermediate, and then reacting the intermediate with thiocyanate to produce the target product prothioconazole. The present method is very specific in terms of regioselectivity, resulting in minimum byproducts and a high product yield. The present method does not require special equipment, nor anhydrous or oxygen-free manipulations. The process is simple and generates minimum wastes, suitable for industrial production.

Abstract: Disclosed are a method of synthesizing prothioconazole and optically active isomers thereof and intermediates. The method includes reacting hydrazine with glyoxylic acid to produce a hydrazono acetic acid as an intermediate, and then reacting the intermediate with thiocyanate to produce the target product prothioconazole. The present method is very specific in terms of regioselectivity, resulting in minimum byproducts and a high product yield. The present method does not require special equipment, nor anhydrous or oxygen-free manipulations. The process is simple and generates minimum wastes, suitable for industrial production.

Abstract: Disclosed is a method of synthesizing 1,2,4-triazole-3-thione compounds and intermediates thereof. The method includes reacting a hydrazine with glyoxylic acid to form a hydrazono acetic acid intermediate followed by reacting the latter with thiocyanate to obtain the 1,2,4-triazole-3-thione compound. The raw materials involved in the present method are readily available, and the reaction is very specific in terms of regioselectivity, resulting in minimum by-product and high product yield. There are neither specific requirements for special equipment nor special operations such as high vacuum, high temperature, anhydrous and oxygen-free manipulations. The process is simple and generates minimum wastes, suitable for industrial production.