Water → (R)-tert-butyl 3-(N-methylcyclopropanesulfonamido)pyrrolidine-1-carboxylate

HRID 527909노트

반응식

HRID 527909 반응식
[CH3:1][NH:2][C@@H:3]1[CH2:7][CH2:6][N:5]([C:8]([O:10][C:11]([CH3:14])([CH3:13])[CH3:12])=[O:9])[CH2:4]1.[CH:15]1([S:18](Cl)(=[O:20])=[O:19])[CH2:17][CH2:16]1.CCN(C(C)C)C(C)C.O>C1COCC1>[CH3:1][N:2]([C@@H:3]1[CH2:7][CH2:6][N:5]([C:8]([O:10][C:11]([CH3:14])([CH3:13])[CH3:12])=[O:9])[CH2:4]1)[S:18]([CH:15]1[CH2:17][CH2:16]1)(=[O:20])=[O:19]

참가 물질

6

반응물 4

HCID 962WaterHCID 81531DiisopropylethylamineHCID 2760919Cyclopropanesulfonyl chlorideHCID 45089543tert-butyl (3R)-3-(methylamino)pyrrolidine-1-carboxylate

생성물 1

HCID 86692139(R)-tert-butyl 3-(N-methylcyclopropanesulfonamido)pyrrolidine-1-carboxylate

시약·촉매·용매 1

HCID 8028Tetrahydrofuran용매

실험 절차

To a solution of (R)-tert-butyl 3-(methylamino)pyrrolidine-1-carboxylate (100 mg, 0.5 mmol) in 2.5 mL THF was added cyclopropanesulfonyl chloride (77 mg, 0.55 mmol) and DIPEA (0.10 mL, 0.60 mmol) at ambient temperature. The mixture was stirred at ambient temperature overnight. Water was added, and then extracted with EtOAc. The organic layers were combined washed with brine, dried over Na2SO4, and evaporated in vacuo to afford the crude title product which was used for the next step without further purification. MS (m/z): 305 (M+H)+.

후처리

  1. extractionextracted with EtOAc
  2. washThe organic layers were combined washed with brine
  3. dry with materialdried over Na2SO4
  4. customevaporated in vacuo

출처 및 근거

ORD 기록
ord-0986bf05a58746b7902fd350e99fefc6
출처 데이터셋
uspto-grants-2016_05
특허 번호
US09346810B2

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