6-fluoro-3-[4-(phenylmethyl)piperazinyl]-1H-indazole → 6-fluoro-3-piperazin-1-yl-1H-indazole

HRID 2051013노트

반응식

HRID 2051013 반응식
[F:1][C:2]1[CH:10]=[C:9]2[C:5]([C:6]([N:11]3[CH2:16][CH2:15][N:14](CC4C=CC=CC=4)[CH2:13][CH2:12]3)=[N:7][NH:8]2)=[CH:4][CH:3]=1.[H][H]>[Ni].[Pd].CO>[F:1][C:2]1[CH:10]=[C:9]2[C:5]([C:6]([N:11]3[CH2:12][CH2:13][NH:14][CH2:15][CH2:16]3)=[N:7][NH:8]2)=[CH:4][CH:3]=1

참가 물질

6

반응물 2

HCID 150574536-fluoro-3-[4-(phenylmethyl)piperazinyl]-1H-indazoleHCID 178418361HCID 178418361, 화합물

생성물 1

HCID 98158716-fluoro-3-piperazin-1-yl-1H-indazole수율 92%

시약·촉매·용매 3

HCID 935Nickel촉매HCID 23938Palladium촉매HCID 887Methanol용매

실험 절차

A mixture of 12 parts of 6-fluoro-3-[4-(phenylmethyl)-piperazinyl]-1H-indazole, 1 part of Raney nickel catalyst and 200 parts of methanol was hydrogenated in a Parr-apparatus at normal pressure and at 50° C. with 2 parts of palladium-on-charcoal catalyst 10%. After the calculated amount of hydrogen was taken up, the catalyst was filtered off over diatomaceous earth and the filtrate was evaporated in vacuo. The residue was crystallized from acetonitrile. The product was filtered off and dried, yielding 7.7 parts (92.0%) of 6-fluoro-3-(1-piperazinyl)-1H-indazole (int. 8).

후처리

  1. filtrationthe catalyst was filtered off over diatomaceous earth
  2. customthe filtrate was evaporated in vacuo
  3. customThe residue was crystallized from acetonitrile
  4. filtrationThe product was filtered off
  5. customdried

출처 및 근거

ORD 기록
ord-e917cc2fee1b4d01aa6d2c9be5496036
출처 데이터셋
uspto-grants-1991_05
특허 번호
US05015740

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