Hydrochloric Acid → (E)-N-{(R)-1-aminomethyl-2-[4-(4-fluoro-phenoxy)-piperidin-1-yl]-ethyl}-3-(5-cyano-2-methoxy-phenyl)-acrylamide

HRID 1797272ノート

反応式

HRID 1797272 の反応式
C(OC(=O)[NH:7][CH2:8][C@@H:9]([NH:25][C:26](=[O:39])/[CH:27]=[CH:28]/[C:29]1[CH:34]=[C:33]([C:35]#[N:36])[CH:32]=[CH:31][C:30]=1[O:37][CH3:38])[CH2:10][N:11]1[CH2:16][CH2:15][CH:14]([O:17][C:18]2[CH:23]=[CH:22][C:21]([F:24])=[CH:20][CH:19]=2)[CH2:13][CH2:12]1)(C)(C)C.Cl>C(Cl)Cl.O1CCOCC1>[NH2:7][CH2:8][C@@H:9]([NH:25][C:26](=[O:39])/[CH:27]=[CH:28]/[C:29]1[CH:34]=[C:33]([C:35]#[N:36])[CH:32]=[CH:31][C:30]=1[O:37][CH3:38])[CH2:10][N:11]1[CH2:16][CH2:15][CH:14]([O:17][C:18]2[CH:19]=[CH:20][C:21]([F:24])=[CH:22][CH:23]=2)[CH2:13][CH2:12]1

参加物

5

反応物 2

HCID 313Hydrochloric AcidHCID 68576228{(R)-2-[(E)-3-(5-cyano-2-methoxy-phenyl)-acryloylamino]-3-[4-(4-fluoro-phenoxy)-piperidin-1-yl]-propyl}-carbamic acid tert-butyl ester

生成物 1

HCID 23566968(E)-N-{(R)-1-aminomethyl-2-[4-(4-fluoro-phenoxy)-piperidin-1-yl]-ethyl}-3-(5-cyano-2-methoxy-phenyl)-acrylamide

試薬・触媒・溶媒 2

HCID 6344Dichloromethane溶媒HCID 312751,4-Dioxane溶媒

実験手順

A solution of {(R)-2-[(E)-3-(5-cyano-2-methoxy-phenyl)-acryloylamino]-3-[4-(4-fluoro-phenoxy)-piperidin-1-yl]-propyl}-carbamic acid tert-butyl ester (0.39 g, 0.71 mmol) in DCM (2 ml) is treated with 4M hydrogen chloride in dioxane (1 ml). The reaction mixture is stirred at room temperature for 1.5 hours and then the solvent evaporated. The residue is co-evaporated with ethanol (×2) to afford (E)-N-{(R)-1-aminomethyl-2-[4-(4-fluoro-phenoxy)-piperidin-1-yl]-ethyl}-3-(5-cyano-2-methoxy-phenyl)-acrylamide.HCl salt. [MH]+ 453.2.

後処理

  1. customthe solvent evaporated

出典と根拠

ORDレコード
ord-1f32b709f16b4d0fb0a816601871eb92
出典データセット
uspto-grants-2006_04
特許番号
US07034042B2

反応ノート

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