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

HRID 1797272노트

반응식

HRID 1797272 반응식
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

참가 물질

5

반응물 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

생성물 1

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

시약·촉매·용매 2

HCID 6344Dichloromethane용매HCID 312751,4-Dioxane용매

실험 절차

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.

후처리

  1. customthe solvent evaporated

출처 및 근거

ORD 기록
ord-1f32b709f16b4d0fb0a816601871eb92
출처 데이터셋
uspto-grants-2006_04
특허 번호
US07034042B2

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