Diisopropylethylamine → (5-Bromo-[1,2,4]triazolo[1,5-a]pyrazin-8-yl)-(3-fluoro-4-morpholin-4-yl-phenyl)-amine

HRID 605906

반응식

HRID 605906 반응식
CN1CCN(C2C=CC(NC3C4N(N=CN=4)C(C4C=C(C(N)=O)SC=4)=CN=3)=CC=2)CC1.[Br:32][C:33]1[N:38]2[N:39]=[CH:40][N:41]=[C:37]2[C:36](Br)=[N:35][CH:34]=1.[F:43][C:44]1[CH:45]=[C:46]([NH2:56])[CH:47]=[CH:48][C:49]=1[N:50]1[CH2:55][CH2:54][O:53][CH2:52][CH2:51]1.CCN(C(C)C)C(C)C>CC(O)C>[Br:32][C:33]1[N:38]2[N:39]=[CH:40][N:41]=[C:37]2[C:36]([NH:56][C:46]2[CH:47]=[CH:48][C:49]([N:50]3[CH2:51][CH2:52][O:53][CH2:54][CH2:55]3)=[C:44]([F:43])[CH:45]=2)=[N:35][CH:34]=1

참가 물질

6

반응물 4

HCID 81531DiisopropylethylamineHCID 14853303-Fluoro-4-morpholinoanilineHCID 497580225,8-Dibromo-(1,2,4)triazolo(1,5-a)pyrazineHCID 575899284-{8-[4-(4-Methyl-piperazin-1-yl)-phenylamino]-[1,2,4]triazolo[1,5-a]pyrazin-5-yl}-thiophene-2-carboxylic acid amide

생성물 1

HCID 57589997(5-Bromo-[1,2,4]triazolo[1,5-a]pyrazin-8-yl)-(3-fluoro-4-morpholin-4-yl-phenyl)-amine수율 98.5%

시약·촉매·용매 1

HCID 3776Isopropanol용매

실험 절차

This compound may be prepared using methods as described for Compound 6, step 1 using 5,8-dibromo-[1,2,4]triazolo[1,5-a]pyrazine (0.5 g, 1.799 mmol), 3-fluoro-4-morpholin-4-yl-phenylamine (0.53 g, 2.70 mmol), and DIPEA (0.470 mL, 2.70 mmol) in 2-propanol (6 mL). The reaction mixture is partitioned between 10% citric acid aqueous solution and DCM. The organic phase is separated and washed with water and brine, dried over MgSO4, filtered and concentrated under vacuum to afford the title compound (697 mg, 98%) which is used in the next step without further purification. LCMS: Rt 3.52 min (98.2%).

후처리

  1. customThis compound may be prepared
  2. customThe reaction mixture is partitioned between 10% citric acid aqueous solution and DCM
  3. customThe organic phase is separated
  4. washwashed with water and brine
  5. dry with materialdried over MgSO4
  6. filtrationfiltered
  7. concentrationconcentrated under vacuum

출처 및 근거

ORD 기록
ord-27112b23025d4d1797f595b435c6a5de
출처 데이터셋
uspto-grants-2011_03
특허 번호
US07915256B2

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