4-[1-(4-Methoxybenzyl)amino-5-isoquinolyl]amino-1-(tert-butoxycarbonyl)piperidine → 4-(1-Amino-5-isoquinolyl)amino-1-(tert-butoxycarbonyl)piperidine

HRID 10581

반응식

HRID 10581 반응식
COC1C=CC(C[NH:8][C:9]2[C:18]3[C:13](=[C:14]([NH:19][CH:20]4[CH2:25][CH2:24][N:23]([C:26]([O:28][C:29]([CH3:32])([CH3:31])[CH3:30])=[O:27])[CH2:22][CH2:21]4)[CH:15]=[CH:16][CH:17]=3)[CH:12]=[CH:11][N:10]=2)=CC=1>FC(F)(F)C(O)=O>[NH2:8][C:9]1[C:18]2[C:13](=[C:14]([NH:19][CH:20]3[CH2:25][CH2:24][N:23]([C:26]([O:28][C:29]([CH3:32])([CH3:31])[CH3:30])=[O:27])[CH2:22][CH2:21]3)[CH:15]=[CH:16][CH:17]=2)[CH:12]=[CH:11][N:10]=1

참가 물질

3

반응물 1

HCID 219799354-[1-(4-Methoxybenzyl)amino-5-isoquinolyl]amino-1-(tert-butoxycarbonyl)piperidine

생성물 1

HCID 219797874-(1-Amino-5-isoquinolyl)amino-1-(tert-butoxycarbonyl)piperidine수율 99.6%

시약·촉매·용매 1

HCID 6422Trifluoroacetic acid용매

실험 절차

A solution of Intermediate 132 (270 mg) in 95% trifluoroacetic acid (5 ml) was stirred at 50° C. for 16 hours, and the solvent was evaporated under reduced pressure. The residue was added with dioxane (3 ml), 2 N aqueous sodium hydroxide (1 ml) and 2 di-t-butyl dicarbonate (393 mg) and stirred at room temperature for 1 hour. The solvent was evaporated under reduced pressure, and then the residue was purified by silica gel column chromatography (n-hexane:ethyl acetate:isopropylamine=5:5:1) to obtain the title compound (199 mg).

후처리

  1. customthe solvent was evaporated under reduced pressure
  2. additionThe residue was added with dioxane (3 ml), 2 N aqueous sodium hydroxide (1 ml) and 2 di-t-butyl dicarbonate (393 mg)
  3. customThe solvent was evaporated under reduced pressure
  4. customthe residue was purified by silica gel column chromatography (n-hexane:ethyl acetate:isopropylamine=5:5:1)

출처 및 근거

ORD 기록
ord-b3e1fac3b5b54f7b92bfe077e81f3e7b
출처 데이터셋
uspto-grants-2006_08
특허 번호
US07094789B2

연결된 노트

불러오는 중…