1-(3-吡咯烷丙基)哌嗪 → 氨

HRID 469122

反应方程式

HRID 469122 反应方程式
[CH:1]1([N:4]([CH2:18][C:19]2[N:23]=[C:22]([C:24]([O:26]CC)=O)[O:21][N:20]=2)[S:5]([C:8]2[C:13]([CH3:14])=[CH:12][C:11]([O:15][CH3:16])=[CH:10][C:9]=2[CH3:17])(=[O:7])=[O:6])[CH2:3][CH2:2]1.[N:29]1([CH2:34][CH2:35][CH2:36][N:37]2[CH2:42][CH2:41][NH:40][CH2:39][CH2:38]2)[CH2:33][CH2:32][CH2:31][CH2:30]1.C[Al](C)C>ClCCCl>[NH3:4].[CH:1]1([N:4]([CH2:18][C:19]2[N:23]=[C:22]([C:24]([N:40]3[CH2:39][CH2:38][N:37]([CH2:36][CH2:35][CH2:34][N:29]4[CH2:30][CH2:31][CH2:32][CH2:33]4)[CH2:42][CH2:41]3)=[O:26])[O:21][N:20]=2)[S:5]([C:8]2[C:13]([CH3:14])=[CH:12][C:11]([O:15][CH3:16])=[CH:10][C:9]=2[CH3:17])(=[O:6])=[O:7])[CH2:3][CH2:2]1

参与物

6

反应物 3

HCID 27372521-(3-吡咯烷丙基)哌嗪HCID 16682925三甲基铝HCID 58393317ethyl 3-({Cyclopropyl[(4-methoxy-2,6-dimethylphenyl)sulfonyl]amino}methyl)-1,2,4-oxadiazole-5-carboxylate

产物 2

HCID 222氨HCID 58393066N-Cyclopropyl-4-methoxy-2,6-dimethyl-N-[(5-{[4-(3-pyrrolidin-1-ylpropyl)piperazin-1-yl]carbonyl}-1,2,4-oxadiazol-3-yl)methyl]benzenesulfonamide

试剂、催化剂与溶剂 1

HCID 111,2-二氯乙烷溶剂

实验过程

The title compound was prepared according to general procedure AT using ethyl 3-({cyclopropyl[(4-methoxy-2,6-dimethylphenyl)sulfonyl]amino}methyl)-1,2,4-oxadiazole-5-carboxylate (30 mg, 0.07 mmol), 1-[3-(pyrrolidin-1-yl)propyl]piperazine (31 mg, 0.16 mmol) and trimethylaluminium (2 M in toluene, 0.07 mL) in DCE (3 mL). The crude product was purified using prep method C, then FCC, eluting with 95:4.5:0.5 DCM:MeOH:NH3, to afford the title compound.

后处理

  1. customThe title compound was prepared
  2. customThe crude product was purified
  3. washFCC, eluting with 95:4.5:0.5 DCM

来源与证据

ORD记录
ord-b80acb4a62ef492b9b35a6545de18922
来源数据集
uspto-grants-2014_01
专利号
US08623859B2

关联笔记

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