Cyano-borohydride → 4-((4-Fluoro-1-(oxetan-3-yl)piperidin-4-yl)methoxy)-3-nitrobenzenesulfonamide

HRID 573201

반응식

HRID 573201 반응식
[F:1][C:2]1([CH2:8][O:9][C:10]2[CH:15]=[CH:14][C:13]([S:16]([NH2:19])(=[O:18])=[O:17])=[CH:12][C:11]=2[N+:20]([O-:22])=[O:21])[CH2:7][CH2:6][NH:5][CH2:4][CH2:3]1.[O:23]1[CH2:26][C:25](=O)[CH2:24]1.C([BH3-])#N>O1CCCC1.C(O)(=O)C>[F:1][C:2]1([CH2:8][O:9][C:10]2[CH:15]=[CH:14][C:13]([S:16]([NH2:19])(=[O:18])=[O:17])=[CH:12][C:11]=2[N+:20]([O-:22])=[O:21])[CH2:7][CH2:6][N:5]([CH:25]2[CH2:26][O:23][CH2:24]2)[CH2:4][CH2:3]1

참가 물질

6

반응물 3

HCID 498716Cyano-borohydrideHCID 150242543-OxetanoneHCID 671265024((4-Fluoropiperidin-4-yl)methoxy)-3-nitrobenzenesulfonamide

생성물 1

HCID 671271554-((4-Fluoro-1-(oxetan-3-yl)piperidin-4-yl)methoxy)-3-nitrobenzenesulfonamide

시약·촉매·용매 2

HCID 176Acetic Acid용매HCID 8028Tetrahydrofuran용매

실험 절차

To a solution of EXAMPLE 341C (72 mg) in tetrahydrofuran (1.5 mL) and acetic acid (0.5 mL) was added oxetan-3-one (14 mg) and MP-cyanoborohydride (2.38 mmol/g, 162 mg). The mixture was stirred at room temperature overnight. The reaction was then filtered and the filtrate was concentrated under vacuum. The residue was slurried in ether and the product was collected by filtration.

후처리

  1. filtrationThe reaction was then filtered
  2. concentrationthe filtrate was concentrated under vacuum
  3. filtrationthe product was collected by filtration

출처 및 근거

ORD 기록
ord-e7b29ce207654796a5a686b34844e679
출처 데이터셋
uspto-grants-2015_05
특허 번호
US09029404B2

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