2-Methoxyethane-1-sulfonyl chloride → N-(3-Fluoro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)-2-methoxyethanesulfonamide

HRID 1052566노트

반응식

HRID 1052566 반응식
[F:1][C:2]1[CH:3]=[C:4]([CH:6]=[C:7]([B:9]2[O:13][C:12]([CH3:15])([CH3:14])[C:11]([CH3:17])([CH3:16])[O:10]2)[CH:8]=1)[NH2:5].[CH3:18][O:19][CH2:20][CH2:21][S:22](Cl)(=[O:24])=[O:23]>N1C=CC=CC=1>[F:1][C:2]1[CH:3]=[C:4]([NH:5][S:22]([CH2:21][CH2:20][O:19][CH3:18])(=[O:24])=[O:23])[CH:6]=[C:7]([B:9]2[O:13][C:12]([CH3:15])([CH3:14])[C:11]([CH3:17])([CH3:16])[O:10]2)[CH:8]=1

참가 물질

4

반응물 2

HCID 134802212-Methoxyethane-1-sulfonyl chlorideHCID 597700393-Fluoro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline

생성물 1

HCID 90102982N-(3-Fluoro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)-2-methoxyethanesulfonamide수율 17%

시약·촉매·용매 1

HCID 1049Pyridine용매

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온도
45 °C

실험 절차

3-Fluoro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline (250 mg, 1.05 mmol) was treated with 2-methoxyethanesulfonyl chloride (326 mg, 2.06 mmol) and 1 ml pyridine as a solvent according to the method described in Preparation 15b but stirring at 45° C. during 3 h. The residue was purified using SP1® Purification System (0% to 100% hexane-ethyl acetate) to obtain 80 mg (17% yield, 81% purity) of the title compound.

후처리

  1. customThe residue was purified
  2. customSP1® Purification System (0% to 100% hexane-ethyl acetate)

출처 및 근거

ORD 기록
ord-67d65dfb55e741f3a0ed456586fdfdc7
출처 데이터셋
uspto-grants-2016_07
특허 번호
US09388189B2

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