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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 661461생성일: 2026년 10월 25일

Hydrochloric Acid → (2R,4S)-4-[(3-Cyano-5-trifluoromethyl-benzyl)-(5-morpholin-4-yl-pyrimidin-2-yl)-amino]-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid tert-butoxycarbonylmethyl ester

https://huagongshe.com/reaction/661461

반응식

참여 물질

역할이름HCID투입량
반응물Hydrochloric AcidHCID 313—
반응물3-(Bromomethyl)-5-(trifluoromethyl)benzonitrileHCID 11601369—
반응물Potassium tert-butoxideHCID 23665647—
반응물(2R,4S)-2-Ethyl-4-(5-morpholin-4-yl-pyrimidin-2-ylamino)-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid tert-butoxycarbonylmethyl esterHCID 67140956—
촉매Tetrabutylammonium IodideHCID 67553—
용매Ethyl AcetateHCID 8857—
용매tert-Butyl methyl etherHCID 15413—
생성물(2R,4S)-4-[(3-Cyano-5-trifluoromethyl-benzyl)-(5-morpholin-4-yl-pyrimidin-2-yl)-amino]-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid tert-butoxycarbonylmethyl esterHCID 86636546—

반응 조건

온도0 °C

반응 단계

The compound obtained in Example 21 (2) above (177 mg) was dissolved in tert-butyl methyl ether (3 ml) under nitrogen atmosphere and the solution was cooled to 0° C. Thereto were added tetrabutylammonium iodide (46 mg), potassium tert-butoxide (105 mg) and 3-Bromomethyl-5-trifluoromethyl-benzonitrile (124 mg), and the mixture was stirred for 2 hours. 1N HCl and ethyl acetate were added to the reaction mixture and the organic layer was separated, washed with a saturated brine, dried over magnesium sulfate and concentrated in vacuo. The resulting residue was purified by column chromatography (NH-silica gel; hexane:ethyl acetate=4:1→3:2) to give the titled compound (39 mg). MS (m/z): 749 [M+H]+.

출처 및 근거

DOI10.6084/m9.figshare.5104873.v1
특허 번호US08084611B2
출처 데이터셋uspto-grants-2011_12
ORD IDord-4ec9e9364d904c84ad2628ee503ff3ce
출처 메모uspto-grants-2011_12