Acetic Acid → 8-Fluoro-5-(4-fluorophenyl)-2,3,4,5-tetrahydro-2-[2-(2-pyridinyl) ethyl]-1H-pyrido[4,3-b]indole

HRID 652473노트

반응식

HRID 652473 반응식
[F:1][C:2]1[CH:10]=[CH:9][C:8]2[N:7]([C:11]3[CH:16]=[CH:15][C:14]([F:17])=[CH:13][CH:12]=3)[C:6]3[CH2:18][CH2:19][NH:20][CH2:21][C:5]=3[C:4]=2[CH:3]=1.[CH:22]([C:24]1[CH:29]=[CH:28][CH:27]=[CH:26][N:25]=1)=[CH2:23].C(O)(=O)C>CO>[F:1][C:2]1[CH:10]=[CH:9][C:8]2[N:7]([C:11]3[CH:12]=[CH:13][C:14]([F:17])=[CH:15][CH:16]=3)[C:6]3[CH2:18][CH2:19][N:20]([CH2:23][CH2:22][C:24]4[CH:29]=[CH:28][CH:27]=[CH:26][N:25]=4)[CH2:21][C:5]=3[C:4]=2[CH:3]=1

참가 물질

5

반응물 3

HCID 176Acetic AcidHCID 75212-VinylpyridineHCID 126299068-fluoro-5-(4-fluorophenyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole

생성물 1

HCID 139003928-Fluoro-5-(4-fluorophenyl)-2,3,4,5-tetrahydro-2-[2-(2-pyridinyl) ethyl]-1H-pyrido[4,3-b]indole수율 89.9%

시약·촉매·용매 1

HCID 887Methanol용매

실험 절차

A mixture of 8-fluoro-5-(4-fluorophenyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole (3 g, 0.01 mole), 2-vinylpyridine (1.7 g, 0.01 mol) and 2 mL of glacial acetic acid were refluxed for 48 hours in 30 mL of methanol. The solvent was removed in vacuo and the separated solid was purified by HPLC using ethyl acetate as the eluant to afford 3.5 g (89.9% yield) of the title compound. It was converted to the dihydrochloride salt; mp. 267°-270° C.

후처리

  1. customThe solvent was removed in vacuo
  2. customthe separated solid was purified by HPLC

출처 및 근거

ORD 기록
ord-3e53e422c9604183b68682d105ec72ec
출처 데이터셋
uspto-grants-1987_06
특허 번호
US04672117

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