Diisopropylethylamine → N4-(5-cyclopropyl-1H-pyrazol-3-yl)-N2-methyl-N2-((1-(tetrahydro-2H-pyran-2-yl)-1H-benzo[d]imidazol-5-yl)methyl)-pyrimidine-2,4-diamine

HRID 475195

반응식

HRID 475195 반응식
Cl[C:2]1[N:7]=[C:6]([NH:8][C:9]2[NH:13][N:12]=[C:11]([CH:14]3[CH2:16][CH2:15]3)[CH:10]=2)[CH:5]=[CH:4][N:3]=1.[CH3:17][NH:18][CH2:19][C:20]1[CH:34]=[CH:33][C:23]2[N:24]([CH:27]3[CH2:32][CH2:31][CH2:30][CH2:29][O:28]3)[CH:25]=[N:26][C:22]=2[CH:21]=1.CCN(C(C)C)C(C)C>CC(O)C>[CH:14]1([C:11]2[NH:12][N:13]=[C:9]([NH:8][C:6]3[CH:5]=[CH:4][N:3]=[C:2]([N:18]([CH3:17])[CH2:19][C:20]4[CH:34]=[CH:33][C:23]5[N:24]([CH:27]6[CH2:32][CH2:31][CH2:30][CH2:29][O:28]6)[CH:25]=[N:26][C:22]=5[CH:21]=4)[N:7]=3)[CH:10]=2)[CH2:16][CH2:15]1

참가 물질

5

반응물 3

HCID 81531DiisopropylethylamineHCID 71272704N-methyl-1-(1-(tetrahydro-2H-pyran-2-yl)-1H-benzo[d]imidazol-5-yl)methanamineHCID 178478345HCID 178478345, 화합물

생성물 1

HCID 86694724N4-(5-cyclopropyl-1H-pyrazol-3-yl)-N2-methyl-N2-((1-(tetrahydro-2H-pyran-2-yl)-1H-benzo[d]imidazol-5-yl)methyl)-pyrimidine-2,4-diamine수율 27.7%

시약·촉매·용매 1

HCID 3776Isopropanol용매

반응 조건

온도
120 °C

실험 절차

A tube was charged with 53 (846 mg, 3.6 mmol), 68 (880 mg, 3.6 mmol), DIPEA (5 mL) and IPA (10 mL), degassed, sealed and then heated at 120° C. overnight. The solvent was evaporated in vacuo to afford 444 mg (27%) N4-(5-cyclopropyl-1H-pyrazol-3-yl)-N2-methyl-N2-((1-(tetrahydro-2H-pyran-2-yl)-1H-benzo[d]imidazol-5-yl)methyl)-pyrimidine-2,4-diamine (70) as a yellow solid; MS (ESI) m/z=445.2 [M+1]+.

후처리

  1. customdegassed
  2. customsealed
  3. customThe solvent was evaporated in vacuo

출처 및 근거

ORD 기록
ord-819352b515fb40c7a38ac84ad72f34b0
출처 데이터셋
uspto-grants-2014_01
특허 번호
US08637537B2

연결된 노트

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