Dimethylformamide → [4-Amino-7-(morpholin-4-ylmethyl)pyrrolo[2,1-f][1,2,4]triazin-6-yl]methanol

HRID 73676노트

반응식

HRID 73676 반응식
CN(C=O)C.[NH2:6][C:7]1[C:12]2=[CH:13][C:14]([CH2:16][OH:17])=[CH:15][N:11]2[N:10]=[CH:9][N:8]=1.[Cl-].[CH2:19]=[N+:20]1[CH2:25][CH2:24][O:23][CH2:22][CH2:21]1>CO>[NH2:6][C:7]1[C:12]2=[CH:13][C:14]([CH2:16][OH:17])=[C:15]([CH2:19][N:20]3[CH2:25][CH2:24][O:23][CH2:22][CH2:21]3)[N:11]2[N:10]=[CH:9][N:8]=1

참가 물질

5

반응물 3

HCID 6228DimethylformamideHCID 11367014Morpholinium, 4-methylene-, chlorideHCID 55297730HCID 55297730, 화합물

생성물 1

HCID 57955268[4-Amino-7-(morpholin-4-ylmethyl)pyrrolo[2,1-f][1,2,4]triazin-6-yl]methanol수율 90%

시약·촉매·용매 1

HCID 887Methanol용매

실험 절차

To a solution of DMF (50 mL) was added (4-aminopyrrolo[2,1-f][1,2,4]triazin-6-yl)methanol (550 mg, 3.35 mmol) and 4-methylenemorpholin-4-ium chloride (Eur. J. Med. Chem. 1989, 24, 379-384) (636 mg, 4.69 mmol). The solution was stirred at rt for 1 h and then the solvent was evaporated. The oil was triturated with CH2Cl2 and a white solid was collected. The free based was obtained by stirring over a Dowex 66 solid support resin in MeOH. The material was filtered and evaporated yielding 794 mg (90%) of the desired product as a white solid. MS [M+H]+=264; LCMS RT=1.07.

후처리

  1. customthe solvent was evaporated
  2. customThe oil was triturated with CH2Cl2
  3. customa white solid was collected
  4. customThe free based was obtained
  5. filtrationThe material was filtered
  6. customevaporated

출처 및 근거

ORD 기록
ord-d984b3b423f440aeb1181f2f44658f6e
출처 데이터셋
uspto-grants-2014_09
특허 번호
US08829185B2

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