反応式
O.O.Cl.[NH2:4][C:5]1[C:14]2[C:9](=[CH:10][C:11]([O:17][CH3:18])=[C:12]([O:15][CH3:16])[CH:13]=2)[N:8]=[C:7]([N:19]2[CH2:24][CH2:23][N:22]([C:25]([CH:27]3[CH2:31][CH2:30][CH2:29][O:28]3)=[O:26])[CH2:21][CH2:20]2)[N:6]=1.NC1C2C(=CC(OC)=C(OC)C=2)N=C([Cl:47])N=1.O1CCCC1C(N1CCNCC1)=O>>[ClH:47].[NH2:4][C:5]1[C:14]2[C:9](=[CH:10][C:11]([O:17][CH3:18])=[C:12]([O:15][CH3:16])[CH:13]=2)[N:8]=[C:7]([N:19]2[CH2:24][CH2:23][N:22]([C:25]([CH:27]3[CH2:31][CH2:30][CH2:29][O:28]3)=[O:26])[CH2:21][CH2:20]2)[N:6]=1参加物
4
実験手順
In its principal embodiment, the present invention comprises a process for the preparation of 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine hydrochloride dihydrate comprising the steps of a) reacting 4-amino-2-chloro-6,7-dimethoxyquinazoline with N-(2-tetrahydrofuroyl)-piperazine in an anhydrous polar organic solvent in the absence of an added acid scavenger to produce the Form IV crystalline modification of anhydrous 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine hydrochloride; and b) thereafter converting the product of Step a) to 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine hydrochloride dihydrate.
出典と根拠
- ORDレコード
- ord-e94674bedc084d458e46f1ba0561a9ad
- 出典データセット
- uspto-grants-1996_04
- 特許番号
- US05504207
関連ノート
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