1-Acetoxy-2-bromoethane → 6-{2-{2-Hydroxyethyl{2-[4-(2-piperidin-1-ylethoxy)phenyl]ethyl}amino}-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol

HRID 1950645노트

반응식

HRID 1950645 반응식
[CH3:1][O:2][C:3]1[CH:8]=[CH:7][C:6]([CH:9]2[CH2:18][CH2:17][C:16]3[CH:15]=[C:14]([O:19]C(=O)C(C)(C)C)[CH:13]=[CH:12][C:11]=3[CH2:10]2)=[C:5]([NH:26][C:27](=O)[CH2:28][C:29]2[CH:34]=[CH:33][C:32]([O:35][CH2:36][CH2:37][N:38]3[CH2:43][CH2:42][CH2:41][CH2:40][CH2:39]3)=[CH:31][CH:30]=2)[CH:4]=1.[H-].[Na+].[C:47](OCCBr)(=[O:49])[CH3:48].[Cl-].[NH4+]>O1CCCC1>[OH:49][CH2:47][CH2:48][N:26]([CH2:27][CH2:28][C:29]1[CH:34]=[CH:33][C:32]([O:35][CH2:36][CH2:37][N:38]2[CH2:39][CH2:40][CH2:41][CH2:42][CH2:43]2)=[CH:31][CH:30]=1)[C:5]1[CH:4]=[C:3]([O:2][CH3:1])[CH:8]=[CH:7][C:6]=1[CH:9]1[CH2:10][CH2:11][C:16]2[CH:15]=[C:14]([OH:19])[CH:13]=[CH:12][C:17]=2[CH2:18]1

참가 물질

6

반응물 4

HCID 135641-Acetoxy-2-bromoethaneHCID 24758Sodium hydrideHCID 25517Ammonium ChlorideHCID 57933831Pivalic acid 6-{4-methoxy-2-{2-[4-(2-piperidin-1-ylethoxy)phenyl]acetylamino}phenyl}-5,6,7,8-tetrahydronaphthalen-2-yl ester

생성물 1

HCID 579341336-{2-{2-Hydroxyethyl{2-[4-(2-piperidin-1-ylethoxy)phenyl]ethyl}amino}-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol

시약·촉매·용매 1

HCID 8028Tetrahydrofuran용매

실험 절차

To a solution of pivalic acid 6-{4-methoxy-2-{2-[4-(2-piperidin-1-ylethoxy)phenyl]acetylamino}phenyl}-5,6,7,8-tetrahydronaphthalen-2-yl ester (30 mg) in tetrahydrofuran (1 ml) was added 60% sodium hydride (2.2 mg), the solution was stirred for 30 minutes at room temperature, then bromoethyl acetate (6.1 μl) was added thereto followed by stirring for 1 hour. To the reaction solution was added a saturated aqueous solution of ammonium chloride, the solution was extracted with chloroform, and concentrated in vacuo. The residue was subjected to the synthetic method of Example 337 described above to provide the title compound (14 mg).

후처리

  1. stirringby stirring for 1 hour
  2. extractionthe solution was extracted with chloroform
  3. concentrationconcentrated in vacuo

출처 및 근거

ORD 기록
ord-f1525b7d3b5842b28739978219944db3
출처 데이터셋
uspto-grants-2013_03
특허 번호
US08399520B2

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