Benzyl 1-(2-(4-(4-acetylpiperazin-1-yl)phenylamino)-5-fluoropyrimidin-4-yl)piperidin-4-ylcarbamate → 1-(4-(4-(4-(4-Aminopiperidin-1-yl)-5-fluoropyrimidin-2-ylamino)phenyl)piperazin-1-yl)ethanone

HRID 2281534노트

반응식

HRID 2281534 반응식
[C:1]([N:4]1[CH2:9][CH2:8][N:7]([C:10]2[CH:15]=[CH:14][C:13]([NH:16][C:17]3[N:22]=[C:21]([N:23]4[CH2:28][CH2:27][CH:26]([NH:29]C(=O)OCC5C=CC=CC=5)[CH2:25][CH2:24]4)[C:20]([F:40])=[CH:19][N:18]=3)=[CH:12][CH:11]=2)[CH2:6][CH2:5]1)(=[O:3])[CH3:2].[H][H]>CO.[Pd]>[NH2:29][CH:26]1[CH2:27][CH2:28][N:23]([C:21]2[C:20]([F:40])=[CH:19][N:18]=[C:17]([NH:16][C:13]3[CH:12]=[CH:11][C:10]([N:7]4[CH2:8][CH2:9][N:4]([C:1](=[O:3])[CH3:2])[CH2:5][CH2:6]4)=[CH:15][CH:14]=3)[N:22]=2)[CH2:24][CH2:25]1

참가 물질

5

반응물 2

HCID 44467167Benzyl 1-(2-(4-(4-acetylpiperazin-1-yl)phenylamino)-5-fluoropyrimidin-4-yl)piperidin-4-ylcarbamateHCID 178418361HCID 178418361, 화합물

생성물 1

HCID 444671681-(4-(4-(4-(4-Aminopiperidin-1-yl)-5-fluoropyrimidin-2-ylamino)phenyl)piperazin-1-yl)ethanone수율 85.5%

시약·촉매·용매 2

HCID 23938Palladium촉매HCID 887Methanol용매

실험 절차

A solution of benzyl 1-(2-(4-(4-acetylpiperazin-1-yl)phenylamino)-5-fluoropyrimidin-4-yl)piperidin-4-ylcarbamate (370 mg, 0.676 mmol) and Pd—C (10%, 55 mg) in MeOH (12 mL) was hydrogenated under balloon hydrogen for 20 h. It was then filtered through celite. The filtrate was concentrated in vacuo to give the titled compound (239 mg). MS 414.3 (M+H); UV 202.8, 268.8 nm.

후처리

  1. filtrationIt was then filtered through celite
  2. concentrationThe filtrate was concentrated in vacuo

출처 및 근거

ORD 기록
ord-1beba1b248f94f2f89a5b7048bad0672
출처 데이터셋
uspto-grants-2015_09
특허 번호
US09139581B2

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