METHOD FOR PRODUCING 3-HALOALKYL PYRAZOLE DERIVATIVE

• Main Authors: SAWAGUCHI MASANORI, MATSUMURA YASUSHI
• Format: Patent
• Language: English; Japanese
• Published: 07.06.2018
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

PROBLEM TO BE SOLVED: To provide a method for producing a 3-haloalkyl pyrazole derivative from an inexpensive raw material compound in a high yield without requiring inefficient separation operation by suppressing the production of isomers.SOLUTION: The method for producing a 3-haloalkyl pyrazole derivative of the following formula (3) comprises reacting a compound of the following formula (1) with a compound of the following formula (2) and then reacting it with a base or an acid. [Ris a 1-6C haloalkyl group; Rand Rare each independently H, a 1-6C alkyl group, a 6-18C aryl group, a 6-26C aryl group having a substituent, a 4-12C heteroaryl group or a 4-30C heteroaryl group having a substituent; X is -CN, -CONRRor COOR; and R, Rand Rare each independently a 1-6C alkyl group.]SELECTED DRAWING: None 【課題】安価な原料化合物から、異性体の生成を抑制し、効率の悪い分離操作を必須とせず、高収率で３−ハロゲン化アルキルピラゾール誘導体を製造する方法の提供。【解決手段】下式（１）の化合物と下式（２）の化合物とを反応させ、次に塩基又は酸と反応させて、下式（３）の３−ハロゲン化アルキルピラゾール誘導体を製造する方法。［Ｒ１はＣ１〜６のハロゲン化アルキル基；Ｒ２及びＲ３は各々独立して、Ｈ、Ｃ１〜６のアルキル基、Ｃ６〜１８のアリール基、置換基を有するＣ６〜２６のアリール基、Ｃ４〜１２のヘテロアリール基又は置換基を有するＣ４〜３０のヘテロアリール基；Ｘは−ＣＮ、−ＣＯＮＲ４Ｒ５又はＣＯＯＲ６；Ｒ４、Ｒ５及びＲ６は各々独立にＣ１〜６のアルキル基］【選択図】なし