1-Hydroxybenzotriazole → (S)-N-(3-Benzyl-3-azabicyclo[3.2.1]oct-8-yl)-4-amino-5-chloro-2-(1-methyl-2-butynyl)oxybenzamide

HRID 936

反応式

HRID 936 の反応式
[NH2:1][C:2]1[C:10]([Cl:11])=[CH:9][C:5]([C:6]([OH:8])=O)=[C:4]([O:12][C@@H:13]([CH3:17])[C:14]#[C:15][CH3:16])[CH:3]=1.N[CH:19]1[CH:24]2[CH2:25][CH2:26][N:20]1[CH2:21][CH:22]([CH2:27][C:28]1C=CC=CC=1)[CH2:23]2.CC[N:36]=C=NCCCN(C)C.Cl.ON1[C:51]2[CH:52]=C[CH:54]=[CH:55][C:50]=2N=N1>>[CH2:26]([N:20]1[CH2:19][CH:24]2[CH:23]([NH:36][C:6](=[O:8])[C:5]3[CH:9]=[C:10]([Cl:11])[C:2]([NH2:1])=[CH:3][C:4]=3[O:12][C@@H:13]([CH3:17])[C:14]#[C:15][CH3:16])[CH:22]([CH2:27][CH2:28]2)[CH2:21]1)[C:25]1[CH:54]=[CH:55][CH:50]=[CH:51][CH:52]=1

参加物

5

反応物 4

HCID 757711-HydroxybenzotriazoleHCID 27239391,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochlorideHCID 15258856(S)-4-amino-5-chloro-2-[(1-methyl-2-butynyl)oxy]benzoic acidHCID 536592488-Amino-3-benzylazabicyclo[3.2.1]octane

生成物 1

HCID 69230097(S)-N-(3-Benzyl-3-azabicyclo[3.2.1]oct-8-yl)-4-amino-5-chloro-2-(1-methyl-2-butynyl)oxybenzamide

実験手順

The condensation of 530 mg of (S)-4-amino-5-chloro-2-[(1-methyl-2-butynyl)oxy]benzoic acid with 850 mg of 8-amino-3-benzylazabicyclo[3.2.1]octane was conducted in a similar manner to that of the Example 34 by the use of WSC.HCl and 1-hydroxybenzotriazole (HOBT). The product was purified by silica gel column chromatography (5% methanol/chloroform) to give 220 mg of the title compound.

後処理

  1. customThe product was purified by silica gel column chromatography (5% methanol/chloroform)

出典と根拠

ORDレコード
ord-9dc5871df86240a4b56e8af07f75976e
出典データセット
uspto-grants-1998_03
特許番号
US05723472

関連ノート

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