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 2075766ノート

反応式

HRID 2075766 の反応式
[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

参加物

5

反応物 3

HCID 6422Trifluoroacetic acidHCID 135975008HCID 135975008、化合物HCID 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

生成物 1

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

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

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.

出典と根拠

ORDレコード
ord-debf975aa58d413b9a1bab830ca2ca06
出典データセット
uspto-grants-2011_04
特許番号
US07923004B2

反応ノート

読み込み中…