Hydrazine hydrate (1:1) → {6-[2-(3-Fluoro-pyridin-2-yl)-imidazol-1-ylmethyl]-5-propyl-pyrimidin-4-yl}-hydrazine

HRID 916650노트

반응식

HRID 916650 반응식
Cl[C:2]1[C:7]([CH2:8][CH2:9][CH3:10])=[C:6]([CH2:11][N:12]2[CH:16]=[CH:15][N:14]=[C:13]2[C:17]2[C:22]([F:23])=[CH:21][CH:20]=[CH:19][N:18]=2)[N:5]=[CH:4][N:3]=1.C(C1C(Cl)=NC=NC=1CBr)CC.FC1C(C2NC=CN=2)=NC=CC=1.O.[NH2:49][NH2:50]>CCO>[F:23][C:22]1[C:17]([C:13]2[N:12]([CH2:11][C:6]3[N:5]=[CH:4][N:3]=[C:2]([NH:49][NH2:50])[C:7]=3[CH2:8][CH2:9][CH3:10])[CH:16]=[CH:15][N:14]=2)=[N:18][CH:19]=[CH:20][CH:21]=1

참가 물질

6

반응물 4

HCID 24654Hydrazine hydrate (1:1)HCID 100423524-Chloro-6-{[2-(3-fluoro-2-pyridinyl)-1H-imidazol-1-yl]methyl}-5-propylpyrimidineHCID 223131604-Bromomethyl-5-propyl-6-chloro-pyrimidineHCID 223131643-Fluoro-2-(1H-imidazol-2-yl)pyridine

생성물 1

HCID 57503304{6-[2-(3-Fluoro-pyridin-2-yl)-imidazol-1-ylmethyl]-5-propyl-pyrimidin-4-yl}-hydrazine

시약·촉매·용매 1

HCID 702Ethanol용매

반응 조건

온도
70 °C

실험 절차

A mixture of 4-chloro-6-[2-(3-fluoro-pyridin-2-yl)-imidazol-1-ylmethyl]-5-propyl-pyrimidine (prepared from 5-propyl-6-bromomethyl-4-chloro-pyrimidine and 3-fluoro-2-(1H-imidazol-2-yl)-pyridine essentially as described in Example 1) (2.5 g, 7.5 mmol) and hydrazine monohydrate (1.37 g, 27.4 mmol) in EtOH (15 mL) is heated in a sealed tube at 70° C. overnight. The solvent is removed in vacuo and the residue is triturated with ethyl acetate and ethyl ether. Filtration gives a white solid (131) which is used in the next step without further purification.

후처리

  1. customThe solvent is removed in vacuo
  2. customthe residue is triturated with ethyl acetate and ethyl ether
  3. filtrationFiltration

출처 및 근거

ORD 기록
ord-6e3a17f9a35e4b42909332e337c702c5
출처 데이터셋
uspto-grants-2007_09
특허 번호
US07271170B2

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