Trifluoroacetic acid → (R)-2-[2-(3-fluorophenyl)-ethyl]pyrrolidine

HRID 928086노트

반응식

HRID 928086 반응식
FC(F)(F)C(O)=O.[F:8][C:9]1[CH:10]=[C:11]([CH2:15][CH2:16][C@@H:17]2[CH2:21][CH2:20][CH2:19][N:18]2C(OC(C)(C)C)=O)[CH:12]=[CH:13][CH:14]=1>C(Cl)Cl>[F:8][C:9]1[CH:10]=[C:11]([CH2:15][CH2:16][C@@H:17]2[CH2:21][CH2:20][CH2:19][NH:18]2)[CH:12]=[CH:13][CH:14]=1

참가 물질

4

반응물 2

HCID 6422Trifluoroacetic acidHCID 71006947tert-butyl (R)-2-[2-(3-fluoro-phenyl)ethyl]pyrrolidine-1-carboxylate2회

생성물 1

HCID 86713377(R)-2-[2-(3-fluorophenyl)-ethyl]pyrrolidine수율 107.6%

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

Trifluoroacetic acid (5 mL) was added to a solution of tert-butyl (R)-2-[2-(3-fluorophenyl)ethyl]-pyrrolidine-1-carboxylate (Intermediate 234, 0.55 g) in DCM (5 mL) and the mixture was stirred at room temperature for 1.5 hours. The mixture was evaporated to dryness and the residue was dissolved in a small amount of methanol and loaded onto a 20 g SCX-2 SPE cartridge, washed with methanol then eluted with 2M ammonia in methanol to give (R)-2-[2-(3-fluorophenyl)-ethyl]pyrrolidine (0.39 g).

후처리

  1. customThe mixture was evaporated to dryness
  2. dissolutionthe residue was dissolved in a small amount of methanol
  3. washwashed with methanol
  4. washthen eluted with 2M ammonia in methanol

출처 및 근거

ORD 기록
ord-ab99dd8489684eb89307c6ddbd499d82
출처 데이터셋
uspto-grants-2016_03
특허 번호
US09290472B2

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