PRODUCTION METHOD OF THIAZOLE DERIVATIVE

• Main Authors: NAKAJO IWAO, YANAGISAWA ARATA, TAGA MASASHI, TADA ATSUSHI, MIMURA AKIHIRO, SUGITA TAKAMASA, AOKI MASASHI
• Format: Patent
• Language: English; Japanese
• Published: 03.12.2020
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

To provide an industrial production method of a thiazole derivative which has an adenosine A2A receptor antagonistic action and is useful as a therapeutic agent for, for example, Parkinson's disease, sleep disorder, analgesic resistance to opioid, migraine, movement disorder, depression, anxiety disorder and the like.SOLUTION: A production method of a compound represented by the formula (C) comprises a step of reacting a compound represented by the formula (A) and a compound represented by the formula (B). (In the formulas, R1 represents furyl; R4 to R6 are the same or different and each represent lower alkyl or aryl; R2 represents pyridyl or tetrahydropyranyl; and X1 represents halogen.)SELECTED DRAWING: None 【課題】アデノシンＡ２Ａ受容体拮抗作用を有し、例えばパーキンソン病、睡眠障害、オピオイドの鎮痛耐性、片頭痛、運動障害、うつ病、不安障害などの治療剤として有用なチアゾール誘導体の工業的製造方法の提供。【解決手段】式（Ａ）で表される化合物と式（Ｂ）で表される化合物を反応させる工程を含む、式（Ｃ）で表される化合物の製造方法。［Ｒ１はフリル；Ｒ４〜Ｒ６はそれぞれ同一又は異なって低級アルキル又はアリール；Ｒ２はピリジル又はテトラヒドロピラニル；Ｘ１はハロゲンを表す］【選択図】なし