Trifluoroacetic acid → Morpholine-3(S)-carboxylic acid {4-[3-(5-chloro-2-hydroxy-phenyl)-1-(2-hydroxy-ethyl)-1H-pyrazol-4-ylethynyl]-phenyl}-amide

HRID 2075766노트

반응식

HRID 2075766 반응식
[Cl:1][C:2]1[CH:3]=[CH:4][C:5]([OH:33])=[C:6]([C:8]2[C:12]([C:13]#[C:14][C:15]3[CH:20]=[CH:19][C:18]([NH:21][C:22]([CH:24]4[CH2:29][O:28][CH2:27][CH2:26][NH:25]4)=[O:23])=[CH:17][CH:16]=3)=[CH:11][N:10]([CH2:30][CH2:31][OH:32])[N:9]=2)[CH:7]=1.C(OC(N1CCOC[C@H]1C(=O)NC1C=CC(C#CC2C(C3C=C(Cl)C=CC=3O)=NN(CCO)C=2)=CC=1)=O)(C)(C)C.C(O)(C(F)(F)F)=O>C(Cl)Cl>[Cl:1][C:2]1[CH:3]=[CH:4][C:5]([OH:33])=[C:6]([C:8]2[C:12]([C:13]#[C:14][C:15]3[CH:20]=[CH:19][C:18]([NH:21][C:22]([C@@H:24]4[CH2:29][O:28][CH2:27][CH2:26][NH:25]4)=[O:23])=[CH:17][CH:16]=3)=[CH:11][N:10]([CH2:30][CH2:31][OH:32])[N:9]=2)[CH:7]=1

참가 물질

5

반응물 3

HCID 6422Trifluoroacetic acidHCID 135975008HCID 135975008, 화합물HCID 1359750093(S)-{4-[3-(5-Chloro-2-hydroxy-phenyl)-1-(2-hydroxy-ethyl)-1H-pyrazol-4-ylethynyl]-phenylcarbamoyl}-morpholine-4-carboxylic acid tert-butyl ester

생성물 1

HCID 135974932Morpholine-3(S)-carboxylic acid {4-[3-(5-chloro-2-hydroxy-phenyl)-1-(2-hydroxy-ethyl)-1H-pyrazol-4-ylethynyl]-phenyl}-amide

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

Using the same procedure for the preparation of 17A, treatment of compound 20A with TFA in methylene chloride to give the title compound 21A as white powder in similar yield. Its 1H NMR and LCMS data are identical with those of compound 17A.

출처 및 근거

ORD 기록
ord-debf975aa58d413b9a1bab830ca2ca06
출처 데이터셋
uspto-grants-2011_04
특허 번호
US07923004B2

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