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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 2234283생성일: 2026년 10월 26일

Water → 3-Methoxy-4-[[2-methyl-6-[(2-methyl1,3-thiazol-4-yl)methyl]-3-oxo-2,6,8,10-tetrazabicyclo[5.4.0]undeca-7,9,11-trien-9-yl]amino]-n-(1-methyl-4-piperidyl)benzamide

https://huagongshe.com/reaction/2234283

반응식

참여 물질

역할이름HCID투입량
반응물WaterHCID 962—
반응물p-Toluenesulfonic acidHCID 6101—
반응물4-Amino-3-methoxy-n-(1-methylpiperidin-4-yl)benzamideHCID 11529063—
반응물10-Chloro-6-methyl-2-[(2-methyl-1,3-thiazol-4-yl)methyl]-2,6,9,11-tetrazabicyclo[5.4.0]undeca-7,9,11-trien-5-oneHCID 86617577—
용매MethanolHCID 887—
용매4-Methyl-2-PentanolHCID 7910—
생성물3-Methoxy-4-[[2-methyl-6-[(2-methyl1,3-thiazol-4-yl)methyl]-3-oxo-2,6,8,10-tetrazabicyclo[5.4.0]undeca-7,9,11-trien-9-yl]amino]-n-(1-methyl-4-piperidyl)benzamideHCID 68684220—

반응 조건

온도160 °C

반응 단계

10-chloro-6-methyl-2-[(2-methyl-1,3-thiazol-4-yl)methyl]-2,6,9,11-tetrazabicyclo[5.4.0]undeca-7,9,11-trien-5-one (Intermediate 101; 58 mg, 0.18 mmol), 4-amino-3-methoxy-N-(1-methyl-4-piperidyl)benzamide (WO06/018220; 49 mg, 0.19 mmol) and p-toluene sulphonic acid (70 mg, 0.37 mmol) were taken up in 4-methyl-2-pentanol (2 mL) and heated to 160° C. in microwave by microwave irradiation for 1 hour. The reaction mixture was dissolved in methanol (5 mL) and water (˜5 mL) and poured directly onto an SCX-3 cartridge (2 g). The cartridge was washed through with methanol (˜30 mL), before elution of products with 2M ammonia in methanol (˜30 mL). Evaporation of the ammoniacal fraction gave an amber film which was purified by reverse phase HPLC to yield the title compound as an off white solid (43 mg, 26%)

출처 및 근거

DOI10.6084/m9.figshare.5104873.v1
특허 번호US07709471B2
출처 데이터셋uspto-grants-2010_05
ORD IDord-ee0da4a715f64827a23937e02a29bf34
출처 메모uspto-grants-2010_05