METHOD FOR PRODUCING 4,4,7-TRIFLUORO-1,2,3,4-TETRAHYDRO-5H-1-BENZAZEPINE COMPOUND AND INTERMEDIATE FOR SYNTHESIS THEREOF

• Main Authors: MIYAFUJI AKIO, AKIBA MASAHIRO, KAWAZOE SOICHIRO, SATO KIICHI, ITO JUNJI, HIRASAWA SHUN, KOHITSU KAZUYOSHI, KOSHIO HIROYUKI
• Format: Patent
• Language: English; Japanese
• Published: 31.01.2019
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; 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 a method for producing a 4,4,7-trifluoro-1,2,3,4-tetrahydro-5H-1-benzazepine compound which has a superior agonistic activity to an arginine vasopressin V2 receptor and is useful as an active ingredient for a pharmaceutical composition for preventing and/or treating urinary frequency, urinary incontinence, enuresis, central diabetes insipidus, nocturia, nocturnal enuresis, or the like; and useful intermediates for use in the production methods.SOLUTION: A production method comprises: a step of reacting a compound of the formula (5) with thionyl chloride (4) to produce a compound of the formula (3); and a step of amidating the compound of the formula (3) by reacting with 2-aminoethanol (2).SELECTED DRAWING: None 【課題】アルギニンバソプレシンV2受容体に対して優れた作動作用を有し、頻尿、尿失禁、遺尿症、中枢性尿崩症、夜間頻尿、夜尿症等の予防及び／又は治療用医薬組成物の有効成分として有用な4,4,7-トリフルオロ-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン化合物の製造方法、及びその製造方法において有用な合成中間体の提供。【解決手段】式（５）の化合物を塩化チオニル（４）と反応させて式（３）の化合物を製造する工程、及び、式（３）の化合物を2-アミノエタノール（２）と反応させアミド化する工程を含む製造方法。【選択図】なし