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HRID 423959作成日:2026年10月24日

L-Phenylalanine, N-[(1,1-dimethylethoxy)carbonyl]- → HCID 178513610、化合物

https://huagongshe.com/ja/reaction/423959

反応式

関与物質

役割名称HCID仕込み量
反応物L-Phenylalanine, N-[(1,1-dimethylethoxy)carbonyl]-HCID 77857—
反応物4-(Bromoacetyl)benzonitrileHCID 98654—
反応物Benzotriazol-1-yloxy-tris(dimethylamino)phosphonium hexafluorophosphateHCID 151348—
反応物Cyano-2-(ethylamino)benzoic acidHCID 66674956—
反応物HCID 178464543HCID 178464543—
溶媒TetrahydrofuranHCID 8028—
溶媒TriethylamineHCID 8471—
生成物HCID 178513610HCID 178513610—

反応手順

Part D: (S)-4-(2-(1-(1-(4-Cyano-2-(ethylamino)phenyl)vinylamino)-2-phenylethyl)-1H-imidazol-4-yl)benzamide: Cyano-2-(ethylamino)benzoic acid from Example 140 Part C (40 mg, 0.2 mmol), Bop reagent (108 mg, 0.24 mmol), and Et3N (0.28 mL) were added together with 5 mL of THF. The mixture was stirred at RT for 15 minutes and (S)-4-(2-(1-Amino-2-phenylethyl)-1H-imidazol-4-yl)benzamide (107 mg, 0.2 mmol), obtained from N-boc-(L)-phenylalanine and 4-(2-Bromo-acetyl)-benzonitrile by the sequential application of the procedures described for Example 1 Part A, Example 28 Part A and Example 1 Part B, was added. The resulting mixture was heated to reflux under N2 for 2 h. The solvent were removed. The residue was dissolved in EtOAc and washed with water and brine. It was dried over MgSO4, concentrated, and purified by ISCO flash chromatography (silica, EtOAc/hexane) to give 50 mg of the desired product. LC/MS: 479.3 (M+1)+.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08101778B2
出典データセットuspto-grants-2012_01
ORD IDord-0a96e639c63c4dcb9f7a0d394d39577a
出典メモuspto-grants-2012_01