Hydrochloric Acid → 4-{2-[2-(Azetidin-1-ylmethyl)pyridin-4-yl]-4-chlorophenoxy}-2,5-difluoro-N-1,3-thiazol-4-ylbenzenesulfonamide

HRID 1692232노트

반응식

HRID 1692232 반응식
[N:1]1([CH2:5][C:6]2[CH:11]=[C:10]([C:12]3[CH:42]=[C:41]([Cl:43])[CH:40]=[CH:39][C:13]=3[O:14][C:15]3[C:20]([F:21])=[CH:19][C:18]([S:22]([N:25]([C:33]4[N:34]=[CH:35][S:36][CH:37]=4)C(=O)OC(C)(C)C)(=[O:24])=[O:23])=[C:17]([F:38])[CH:16]=3)[CH:9]=[CH:8][N:7]=2)[CH2:4][CH2:3][CH2:2]1.Cl>ClCCl.O1CCOCC1>[N:1]1([CH2:5][C:6]2[CH:11]=[C:10]([C:12]3[CH:42]=[C:41]([Cl:43])[CH:40]=[CH:39][C:13]=3[O:14][C:15]3[C:20]([F:21])=[CH:19][C:18]([S:22]([NH:25][C:33]4[N:34]=[CH:35][S:36][CH:37]=4)(=[O:23])=[O:24])=[C:17]([F:38])[CH:16]=3)[CH:9]=[CH:8][N:7]=2)[CH2:2][CH2:3][CH2:4]1

참가 물질

5

반응물 2

HCID 313Hydrochloric AcidHCID 59436494tert-Butyl [(4-{2-[2-(azetidin-1-ylmethyl)pyridin-4-yl]-4-chlorophenoxy}-2,5-difluorophenyl)sulfonyl]1,3-thiazol-4-ylcarbamate

생성물 1

HCID 468419354-{2-[2-(Azetidin-1-ylmethyl)pyridin-4-yl]-4-chlorophenoxy}-2,5-difluoro-N-1,3-thiazol-4-ylbenzenesulfonamide

시약·촉매·용매 2

HCID 6344Dichloromethane용매HCID 312751,4-Dioxane용매

실험 절차

tert-Butyl [(4-{2-[2-(azetidin-1-ylmethyl)pyridin-4-yl]-4-chlorophenoxy}-2,5-difluorophenyl)sulfonyl]1,3-thiazol-4-ylcarbamate, (Preparation 878, 0.325 g, 0.0005 mol) was dissolved in dichloromethane (3 mL) then 4 molar hydrogen chloride in 1,4-dioxane (3 mL) was added. The reaction was stirred at room temperature for 18 hours. The reaction was concentrated in vacuo and the crude product purified by preparative HPLC to give the title compound.

후처리

  1. concentrationThe reaction was concentrated in vacuo
  2. customthe crude product purified by preparative HPLC

출처 및 근거

ORD 기록
ord-228b304eddd94e489c5e176fc4891da5
출처 데이터셋
uspto-grants-2012_04
특허 번호
US08153814B2

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