反応式
[CH3:1][C@H:2]1[C@:19]([OH:24])([C:20]([CH2:22][OH:23])=[O:21])[C@:18]2([CH3:25])[C@H:4]([C@H:5]3[C@:15](F)([C@@H:16]([OH:26])[CH2:17]2)[C@:14]2([CH3:28])[C:8](=[CH:9][C:10]([CH:12]=[CH:13]2)=[O:11])[CH2:7][CH2:6]3)[CH2:3]1.O[C@@]1([C@]2(C)[C@H]([C@H]3C(=CC2)[C@]2(C)C(=CC(=O)C=C2)CC3)CC1=C)C(=O)C>>[O:26]1[C@@H:16]2[C@:15]31[C@H:5]([C@H:4]1[C@:18]([CH3:25])([CH2:17]2)[C@@:19]([OH:24])([C:20](=[O:21])[CH2:22][OH:23])[C@H:2]([CH3:1])[CH2:3]1)[CH2:6][CH2:7][C:8]1[C@:14]3([CH3:28])[CH:13]=[CH:12][C:10](=[O:11])[CH:9]=1参加物
実験手順
Dexamethasone (9α-fluoro-11β,17α,21-trihydroxy-16α-methylpregna-1,4-diene-3,20-dione) can also be prepared from 17β-hydroxy-16-methylenepregna-1,4,9(11)-triene-3,20-dione (VIIB, Example 18) by first transforming it to 17α,21-dihydroxy-16-methylenepregna-1,4,9(11)-triene-3,20-dione 21-acetate (IX) as described above and next transforming it to 17α,21-dihydroxy-16α-methylpregna-1,4,9(11)-triene-3,20-dione 21-acetate (XI) by the process of U.S. Pat. No. 3,130,209. 17α,21-Dihydroxy-16α-methylpregna-1,4,9(11)-triene-3,20-dioine 21-acetate (XI) is then epoxidized by means well known to those skilled in the art, see for example U.S. Pat. No. 3,980,778 Examples 2 and 7 to produce 9β,11β-epoxy-17α,21-dihydroxy-16α-methylpregna-1,4-diene-3,20-dione which is transformed to dexamethasone 21-acetate by the process of U.S. Pat. No. 3,007,923 Example 2.
出典と根拠
- ORDレコード
- ord-82c6899d60234582bdf3d1fbfa578039
- 出典データセット
- uspto-grants-1986_01
- 特許番号
- US04567001
関連ノート
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