Picolinoyl Chloride Hydrochloride → HCID 86664022, 화합물

HRID 712309

반응식

HRID 712309 반응식
[NH2:1][C:2]1[C:10]2[S:9][C:8]([NH:11][C:12]([NH:14][CH2:15][CH3:16])=[O:13])=[N:7][C:6]=2[CH:5]=[C:4]([C:17]2[CH:18]=[N:19][C:20]([N:23]3[CH2:28][CH2:27][C:26]([CH3:34])([C:29]([O:31][CH2:32][CH3:33])=[O:30])[CH2:25][CH2:24]3)=[N:21][CH:22]=2)[CH:3]=1.Cl.[N:36]1[CH:41]=[CH:40][CH:39]=[CH:38][C:37]=1[C:42](Cl)=[O:43]>N1C=CC=CC=1>[CH2:15]([NH:14][C:12](=[O:13])[NH:11][C:8]1[S:9][C:10]2[C:2]([NH:1][C:42](=[O:43])[C:37]3[CH:38]=[CH:39][CH:40]=[CH:41][N:36]=3)=[CH:3][C:4]([C:17]3[CH:18]=[N:19][C:20]([N:23]4[CH2:24][CH2:25][C:26]([CH3:34])([C:29]([O:31][CH2:32][CH3:33])=[O:30])[CH2:27][CH2:28]4)=[N:21][CH:22]=3)=[CH:5][C:6]=2[N:7]=1)[CH3:16]

참가 물질

4

반응물 2

HCID 135033Picolinoyl Chloride HydrochlorideHCID 86664019Ethyl 1-(5-(7-amino-2-(3-ethylureido)benzo[d]thiazol-5-yl)pyrimidin-2-yl)-4-methylpiperidine-4-carboxylate

생성물 1

HCID 86664022HCID 86664022, 화합물수율 68%

시약·촉매·용매 1

HCID 1049Pyridine용매

실험 절차

Ethyl 1-(5-(7-amino-2-(3-ethylureido)benzo[d]thiazol-5-yl)pyrimidin-2-yl)-4-methylpiperidine-4-carboxylate (119 mg, 0.25 mmol) was dissolved in pyridine (2 ml) then picolinoyl chloride hydrochloride (58 mg, 0.33 mmol) was added with stirring and the reaction stirred at rt for 18 h. The pyridine was removed under reduced pressure and the residue triturated with water. The resulting solid was collected by filtration and dried to afford the crude product 100 mg (68%). This material was used directly in the next step without further purification.

후처리

  1. stirringthe reaction stirred at rt for 18 h
  2. customThe pyridine was removed under reduced pressure
  3. customthe residue triturated with water
  4. filtrationThe resulting solid was collected by filtration
  5. customdried

출처 및 근거

ORD 기록
ord-277f3e01570845bfb258ebfe078f5730
출처 데이터셋
uspto-grants-2015_11
특허 번호
US09181234B2

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