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PROBLEM TO BE SOLVED: To provide a method of producing 6-(2,6-dimethylpyrimidin-4-yl)-N-(4-(ethylsulfonyl)benzyl)-6-methyl-5-oxo-5,6,7,8-tetrahydroquinoline-2-carboxamide, which is a retinoic acid receptor-related orphan receptor (ROR) modulator, effective for an immune or inflammatory disease.
SOLUTION: There is provided a process of preparing a compound according to the following scheme, which includes coupling a carboxylic acid with an amine in the presence of a base and a coupling agent, and isolating a desired product from the reaction mixture, and may additionally include chiral separation of the compound for isolating an enantiomer.
SELECTED DRAWING: None
COPYRIGHT: (C)2020,JPO&INPIT
【課題】免疫疾患や炎症性疾患に有効な、レチノイン酸受容体関連オーファン受容体(ROR)調節物質である、6−(2,6−ジメチルピリミジン−4−イル)−N−(4−(エチルスルホニル)ベンジル)−6−メチル−5−オキソ−5,6,7,8−テトラヒドロキノリン−2−カルボキサミドの製造方法の提供。【解決手段】以下のスキームに従って化合物を調製するプロセスであって、塩基及びカップリング剤の存在下でカルボン酸をアミンとカップリングする工程、及び反応混合物から所望の生成物の単離する工程を含む、プロセス。エナンチオマーを単離するために化合物のキラル分離の追加の工程を含んでいても良い。【選択図】なし