反応式
[Cl:1]C1C(Cl)=C(C)C=CC=1N.C(NC1C=CC=CC=1)=O.OCCN.[CH2:24]1[C:28]2([NH:36][C:31]3([CH2:35][CH2:34][CH2:33][CH2:32]3)[CH2:30][O:29]2)[CH2:27][CH2:26][CH2:25]1.O1CCNC1>>[ClH:1].[OH:29][CH2:30][C:31]1([NH2:36])[CH2:35][CH2:34][CH2:33][CH2:32]1.[CH:28]1([NH:36][C:31]2([CH2:30][OH:29])[CH2:35][CH2:34][CH2:33][CH2:32]2)[CH2:24][CH2:25][CH2:26][CH2:27]1参加物
実験手順
2,3-Dichloro-4-methylaniline was converted to the 2,3-dichloro-4-methylformanilide according to Method A3a, Step 1. The formanilide was converted to 2,3-dichloro-4-methylphenyl isocyanide dichloride according to Method A3a, Step 2. 1-Hydroxymethylcyclopentanamine HCl salt was synthesized according to Method B1c. The 2-hydroxyethylamine was converted to 13-aza-6-oxadispiro[4.2.4.1]tridecane according to Method B4d, Step 1. The oxazolidine was reductively opened according to Method B4d, Step 2 to give 1-(cyclopentylamino)-1-(hydroxymethyl)cyclopentane. The substituted 2-hydroxyethylamine was converted to 1-(cyclopentylamino)-1-(thioacetylmethyl)cyclopentane according to Method C6c, Step 1. The thioacetate was hydrolyzed according to Method C6c, Step 2 to give 1-(cyclopentylamino)-1-(thiomethyl)cyclopentane. The 2-thioethylamine was reacted with 2,3-dichloro-4-methylphenyl isocyanide dichloride according to Method C6c to afford 2-(2,3-dichloro-4-methylphenylimino)-1-cyclopentyl-3-thia-1-azaspiro[4.4]nonane.
出典と根拠
- ORDレコード
- ord-983633fdaaa444cab915f9738f7cee4c
- 出典データセット
- uspto-grants-2002_03
- 特許番号
- US06353006B1
関連ノート
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