HCID 86601761, 화합물 → HCID 178451099, 화합물

HRID 1162550노트

반응식

HRID 1162550 반응식
Br[CH2:2][C:3]([C:5]1[CH:10]=[CH:9][C:8]([O:11][C@H:12]2[CH2:17][CH2:16][C@H:15]([CH3:18])[CH2:14][CH2:13]2)=[CH:7][CH:6]=1)=O.[C:19]([O:23][C:24](=[O:36])[CH2:25][CH2:26][N:27]([CH:31]1[CH2:35][CH2:34][CH2:33][CH2:32]1)[C:28]([NH2:30])=[S:29])([CH3:22])([CH3:21])[CH3:20]>CN1C(=O)CCC1>[C:19]([O:23][C:24](=[O:36])[CH2:25][CH2:26][N:27]([CH:31]1[CH2:35][CH2:34][CH2:33][CH2:32]1)[C:28]1[S:29][CH:2]=[C:3]([C:5]2[CH:10]=[CH:9][C:8]([O:11][C@H:12]3[CH2:17][CH2:16][C@H:15]([CH3:18])[CH2:14][CH2:13]3)=[CH:7][CH:6]=2)[N:30]=1)([CH3:22])([CH3:20])[CH3:21]

참가 물질

4

반응물 2

HCID 86601761HCID 86601761, 화합물HCID 178461403HCID 178461403, 화합물

생성물 1

HCID 178451099HCID 178451099, 화합물수율 88.1%

시약·촉매·용매 1

HCID 13387N-methyl-2-pyrrolidone용매

실험 절차

The 2-bromo-1-[4-(trans-4-methyl-cyclohexyloxy)-phenyl]-ethanone (764 mg, 3.44 mmol), 3-(1-cyclopentyl-thioureido)-propionic acid tert-butyl ester (935 mg, 2.46 mmol), NMP (6 mL) were combined as indicated in general procedure B. The reaction was stirred at room temperature overnight. After an aqueous work up, the crude product was purified by silica gel chromatography (gradient, hexane→3% EtOAc-hexane) to afford 3-(cyclopentyl-{4-[4-(trans-4-methyl-cyclohexyloxy)-phenyl]-thiazol-2-yl}-amino)-propionic acid tert-butyl ester (1.05 g).

후처리

  1. customAfter an aqueous work up, the crude product was purified by silica gel chromatography (gradient, hexane→3% EtOAc-hexane)

출처 및 근거

ORD 기록
ord-eee50094ff82441c99f1d1c3d26c2c7b
출처 데이터셋
uspto-grants-2010_10
특허 번호
US07820704B2

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