1-Hydroxybenzotriazole → tert-Butyl cis(+/-)-4-{[(4,5-diiodo-1H-imidazol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-carboxylate

HRID 1424998

反応式

HRID 1424998 の反応式
[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].[I:17][C:18]1[N:19]=[C:20]([C:24](O)=[O:25])[NH:21][C:22]=1[I:23].CCN=C=NCCCN(C)C.Cl.C1C=CC2N(O)N=NC=2C=1>>[I:17][C:18]1[N:19]=[C:20]([C:24]([NH:1][C@H:2]2[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]2[O:15][CH3:16])=[O:25])[NH:21][C:22]=1[I:23]

参加物

5

反応物 4

HCID 757711-HydroxybenzotriazoleHCID 27239391,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochlorideHCID 57362389(3R,4S)-4-Amino-1-boc-3-methoxypiperidine2 回HCID 675484814,5-diiodo-1H-imidazole-2-carboxylic acid

生成物 1

HCID 86648535tert-Butyl cis(+/-)-4-{[(4,5-diiodo-1H-imidazol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-carboxylate収率 43%

実験手順

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) (170 mg, 0.74 mmol), 4,5-diiodoimidazole-2-carboxylic acid obtained in Example (71b) (about 0.34 mmol), WSC hydrochloride (195 mg, 1.02 mmol) and HOBT (46 mg, 0.34 mmol), to obtain 83.1 mg of the title compound as a white solid (43%).

後処理

  1. customobtained by the method

出典と根拠

ORDレコード
ord-00edae6b02ae49fca81733d7c2bc02be
出典データセット
uspto-grants-2015_01
特許番号
US08927588B2

関連ノート

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