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1H-Imidazole-2-carboxylic acid → tert-Butyl cis(+/-)-4-[(1H-imidazol-2-ylcarbonyl)amino]-3-methoxypiperidine-1-carboxylate

HRID 43436
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인쇄 미리보기

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HRID 43436 반응식
[NH2:1][C@H:2]1[CH2:7][CH2:6][N:5]([C:8]([O:10][C:11]([CH3:14])([CH3:13])[CH3:12])=[O:9])[CH2:4][C@H:3]1[O:15][CH3:16].[NH:17]1[CH:21]=[CH:20][N:19]=[C:18]1[C:22](O)=[O:23].CCN=C=NCCCN(C)C.Cl>CN(C1C=CN=CC=1)C>[NH:17]1[CH:21]=[CH:20][N:19]=[C:18]1[C:22]([NH:1][C@H:2]1[CH2:7][CH2:6][N:5]([C:8]([O:10][C:11]([CH3:12])([CH3:13])[CH3:14])=[O:9])[CH2:4][C@H:3]1[O:15][CH3:16])=[O:23]
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참가 물질

5

반응물 3

HCID 5743211H-Imidazole-2-carboxylic acidHCID 27239391,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochlorideHCID 57362389(3R,4S)-4-Amino-1-boc-3-methoxypiperidine2회

생성물 1

HCID 86648456tert-Butyl cis(+/-)-4-[(1H-imidazol-2-ylcarbonyl)amino]-3-methoxypiperidine-1-carboxylate수율 58%

시약·촉매·용매 1

HCID 14284
4-(Dimethylamino)pyridine
촉매

실험 절차

The same operation as in Example (1g) was performed using tert-butyl cis(±)-4-amino-3-methoxypiperidine-1-carboxylate obtained by the method described in Example (1e) (0.20 g, 0.87 mmol), 1H-imidazole-2-carboxylic acid obtained in Example (3a) (91 mg, 0.81 mmol), WSC hydrochloride (0.36 g, 1.88 mmol) and DMAP (10 mg, 0.083 mmol), to obtain 138 mg of the title compound as a white solid (58%).

후처리

  1. customobtained by the method

출처 및 근거

ORD 기록
ord-ce31ef13e58f4c2e8194f2fc1e24d25f
출처 데이터셋
uspto-grants-2013_09
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US08536197B2

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