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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 446498생성일: 2026년 10월 24일

Toluene → 1-{2-[{6-[({5-[{3-[({[(2S)-1'-{2-[(5R)-3-[3,5-Bis(trifluoromethyl)benzoyl]-5-(4-fluorophenyl)-1,3-oxazolidin-5-yl]ethyl}-2,3-dihydrospiro[indene-1,4'-piperidin]-2-yl]oxy}acetyl)(methyl)amino]propyl}(methyl)carbamoyl]-2-thienyl}methyl)amino]hexanoyl}(methyl)amino]ethyl}piperidin-4-yl biphenyl-2-ylcarbamate

https://huagongshe.com/ko/reaction/446498

반응식

참여 물질

역할이름HCID투입량
반응물TolueneHCID 1140—
반응물Sodium triacetoxyborohydrideHCID 5049666—
반응물1-{2-[(6-Aminohexanoyl)(methyl)amino]ethyl}piperidin-4-yl biphenyl-2-ylcarbamateHCID 66671572—
반응물N-{3-[({[(2S)-1'-{2-[(5R)-3-[3,5-Bis(trifluoromethyl)benzoyl]-5-(4-fluorophenyl)-1,3-oxazolidin-5-yl]ethyl}-2,3-dihydrospiro[indene-1,4'-piperidin]-2-yl]oxy}acetyl)(methyl)amino]propyl}-5-formyl-N-methylthiophene-2-carboxamideHCID 86663421—
용매MethanolHCID 887—
생성물Ammonium AcetateHCID 5171650.1%
생성물1-{2-[{6-[({5-[{3-[({[(2S)-1'-{2-[(5R)-3-[3,5-Bis(trifluoromethyl)benzoyl]-5-(4-fluorophenyl)-1,3-oxazolidin-5-yl]ethyl}-2,3-dihydrospiro[indene-1,4'-piperidin]-2-yl]oxy}acetyl)(methyl)amino]propyl}(methyl)carbamoyl]-2-thienyl}methyl)amino]hexanoyl}(methyl)amino]ethyl}piperidin-4-yl biphenyl-2-ylcarbamateHCID 4692929653.1%

반응 단계

The compound (73 mg, 0.157 mmol) obtained in Example 1a and the compound (144 mg, 0.157 mmol) obtained in Example 1l were dissolved in methanol (2 mL), and the mixture was stirred at room temperature for 15 minutes. Toluene was added, then the solvent was evaporated under reduced pressure, sodium triacetoxyborohydride (100 mg, 0.471 mmol) was added to a solution of the resulting residue in methanol (2 mL), and the mixture was stirred at room temperature for 2.5 hours. The solvent was evaporated under reduced pressure, and the resulting residue was purified by NH silica gel column chromatography (ethyl acetate:methanol=60:1→20:1, v/v) and further purified by reverse phase preparative column chromatography (Waters; XTerra Prep MS C18 OBD, 5 μm, 30×100 mm) (acetonitrile:0.1% aqueous ammonium acetate solution=40:60→100:0, v/v) to give the title compound (57 mg; yield, 27%) as a light yellow solid.

출처 및 근거

DOI10.6084/m9.figshare.5104873.v1
특허 번호US08476253B2
출처 데이터셋uspto-grants-2013_07
ORD IDord-6e891253fcb44f4384c50f4d1ce20e8f
출처 메모uspto-grants-2013_07