1,2,3,6-Tetrahydropyridine → 1-(1,3-Benzoxazol-6-ylcarbonyl)-1,2,3,6-tetrahydropyridine
反応式
[O:1]1[C:5]2[CH:6]=[C:7]([C:10]([OH:12])=O)[CH:8]=[CH:9][C:4]=2[N:3]=[CH:2]1.[NH:13]1[CH2:18][CH:17]=[CH:16][CH2:15][CH2:14]1.C(C1NC=CN=1)(C1NC=CN=1)=O.C(Cl)(=O)C(Cl)=O>>[O:1]1[C:5]2[CH:6]=[C:7]([C:10]([N:13]3[CH2:14][CH:15]=[CH:16][CH2:17][CH2:18]3)=[O:12])[CH:8]=[CH:9][C:4]=2[N:3]=[CH:2]1参加物
5
実験手順
Coupling of 1,3-benzoxazol-6-carboxylic acid with 1,2,3,6-tetrahydropyridine is performed in the same manner as described for the preparation of Invention Compound V through activation with carbonyl diimidazole or by activation with other suitable reagents such as oxalyl chloride. The product can be isolated by the same methods as described for the isolation of Invention Compound V and purified by chromatography on silica gel. EIMS m/z=228 (parent), 146 (base), and 118. 1H NMR δ 2.2 (br, 2), 3.4-4.3 (br m, 4), 5.7-5.95 (br m, 2), 7.52 (dd, 1, J=8.39, 1.49 Hz), 7.64 (d, 1, J=8.41 Hz), 7.87 (d, 1, J=1.32 Hz), and 8.16 ppm (s, 1).
後処理
- customThe product can be isolated by the same methods
- custompurified by chromatography on silica gel
出典と根拠
- ORDレコード
- ord-7b06e1cf9a5e4616abe2c06d9171acd0
- 出典データセット
- uspto-grants-1999_04
- 特許番号
- US05891876
反応ノート
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