1,2,3,6-Tetrahydropyridine → 1-(1,3-Benzoxazol-6-ylcarbonyl)-1,2,3,6-tetrahydropyridine

HRID 1458524ノート

反応式

HRID 1458524 の反応式
[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

反応物 4

HCID 127501,2,3,6-TetrahydropyridineHCID 65578Oxalyl chlorideHCID 5250894Bis-(1H-imidazol-2-YL)-methanoneHCID 222459381,3-Benzoxazole-6-carboxylic acid

生成物 1

HCID 115359401-(1,3-Benzoxazol-6-ylcarbonyl)-1,2,3,6-tetrahydropyridine

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

  1. customThe product can be isolated by the same methods
  2. custompurified by chromatography on silica gel

出典と根拠

ORDレコード
ord-f2e3669a41164b1d8b7e7dc19d7320ae
出典データセット
uspto-grants-1998_12
特許番号
US05852008

反応ノート

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