1,4,5,6-Tetrahydropyrimidin-2-amine → (2s)-2-(1-Adamantylmethoxycarbonylamino)-3-((5-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)-cyclopropyl)-thiophene-2-carbonyl)-amino)-propionic acid tert-butyl ester

HRID 431511ノート

反応式

HRID 431511 の反応式
C[O:2][C:3]([CH:5]1[CH2:7][CH:6]1[C:8]1[S:9][C:10]([C:13](=[O:39])[NH:14][CH2:15][C@H:16]([NH:24][C:25]([O:27][CH2:28][C:29]23[CH2:38][CH:33]4[CH2:34][CH:35]([CH2:37][CH:31]([CH2:32]4)[CH2:30]2)[CH2:36]3)=[O:26])[C:17]([O:19][C:20]([CH3:23])([CH3:22])[CH3:21])=[O:18])=[CH:11][CH:12]=1)=O.[NH2:40][C:41]1[NH:42][CH2:43][CH2:44][CH2:45][N:46]=1>CN(C)C=O>[C:20]([O:19][C:17](=[O:18])[C@@H:16]([NH:24][C:25]([O:27][CH2:28][C:29]12[CH2:38][CH:33]3[CH2:32][CH:31]([CH2:37][CH:35]([CH2:34]3)[CH2:36]1)[CH2:30]2)=[O:26])[CH2:15][NH:14][C:13]([C:10]1[S:9][C:8]([CH:6]2[CH2:7][CH:5]2[C:3](=[O:2])[NH:40][C:41]2[NH:46][CH2:45][CH2:44][CH2:43][N:42]=2)=[CH:12][CH:11]=1)=[O:39])([CH3:21])([CH3:23])[CH3:22]

参加物

4

反応物 2

HCID 32874121,4,5,6-Tetrahydropyrimidin-2-amineHCID 572486992-(5-(((2s)-2-(1-Adamantylmethoxycarbonylamino)-2-tert-butoxycarbonyl-ethyl)carbamoyl)-2-thienyl)-cyclopropancarboxylic acid methyl ester

生成物 1

HCID 69637307(2s)-2-(1-Adamantylmethoxycarbonylamino)-3-((5-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)-cyclopropyl)-thiophene-2-carbonyl)-amino)-propionic acid tert-butyl ester

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

The product obtained in step b) was dissolved in 4 ml of anhydrous dimethylformamide and stirred under an argon atmosphere with 99 mg of 2-amino-1,4,5,6-tetrahydropyrimidine for 7 hours at room temperature. The solvent was removed in vacuo and the residue was chromatographed (silica gel; ethyl acetate/methanol (1/1, v/v)). The fractions containing the title compound were pooled and evaporated under reduced pressure to give 53 mg of a colourless resin.

後処理

  1. customThe solvent was removed in vacuo
  2. customthe residue was chromatographed (silica gel
  3. additionThe fractions containing the title compound
  4. customevaporated under reduced pressure

出典と根拠

ORDレコード
ord-9152ad8f8b2647a3a50b0fda14815517
出典データセット
uspto-grants-2003_12
特許番号
US06660728B2

反応ノート

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