Amlodipine → 2-[2-(-(S)-4-Benzyloxycarbonylamino-4-methoxycarbonylbutanamido)ethoxymethyl]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine

HRID 1382624ノート

反応式

HRID 1382624 の反応式
[NH2:1][CH2:2][CH2:3][O:4][CH2:5][C:6]1[NH:7][C:8]([CH3:28])=[C:9]([C:24]([O:26][CH3:27])=[O:25])[CH:10]([C:17]2[CH:22]=[CH:21][CH:20]=[CH:19][C:18]=2[Cl:23])[C:11]=1[C:12]([O:14][CH2:15][CH3:16])=[O:13].[CH2:29]([O:36][C:37]([NH:39][C@H:40]([C:46]([O:48][CH3:49])=[O:47])[CH2:41][CH2:42][C:43](O)=[O:44])=[O:38])[C:30]1[CH:35]=[CH:34][CH:33]=[CH:32][CH:31]=1.Cl.CN(C)CCCN=C=NCC.ON1C2C=CC=CC=2N=N1>ClCCl.C(N(CC)CC)C>[CH2:29]([O:36][C:37]([NH:39][C@H:40]([C:46]([O:48][CH3:49])=[O:47])[CH2:41][CH2:42][C:43]([NH:1][CH2:2][CH2:3][O:4][CH2:5][C:6]1[NH:7][C:8]([CH3:28])=[C:9]([C:24]([O:26][CH3:27])=[O:25])[CH:10]([C:17]2[CH:22]=[CH:21][CH:20]=[CH:19][C:18]=2[Cl:23])[C:11]=1[C:12]([O:14][CH2:15][CH3:16])=[O:13])=[O:44])=[O:38])[C:30]1[CH:31]=[CH:32][CH:33]=[CH:34][CH:35]=1

参加物

7

反応物 4

HCID 2162AmlodipineHCID 757711-HydroxybenzotriazoleHCID 27239391,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochlorideHCID 2733408(4S)-4-{[(benzyloxy)carbonyl]amino}-5-methoxy-5-oxopentanoic acid

生成物 1

HCID 228414672-[2-(-(S)-4-Benzyloxycarbonylamino-4-methoxycarbonylbutanamido)ethoxymethyl]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine収率 74%

試薬・触媒・溶媒 2

HCID 6344Dichloromethane溶媒HCID 8471Triethylamine溶媒

実験手順

A mixture of 2-[2-aminoethoxymethyl]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine (1.61 g), ("amlodipine"), (S)-4-benzyloxycarbonylamino-4-methoxycarbonylbutanoic acid (1.28 g) [see G. H. L. Nefkens and J. F. Nivard, Rec. Trav. Chim. Pays Bas, 199, 83, 1964], 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (0.83 g), 1-hydroxybenzotriazole (0.59 g) and triethylamine (0.44 g) in dichloromethane (25 ml) were reacted together as described in Example 5 part (a) to give the title compound (2.0 g) as an essentially pure solid foam which was used directly in Example 1 and Preparation 2 without further purification.

後処理

  1. customwere reacted together

出典と根拠

ORDレコード
ord-502a78c8ade34dfc9beb268d07f8c9fd
出典データセット
uspto-grants-1989_02
特許番号
US04806557

反応ノート

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