[8-(5-p-Methylphenyloxazol-2-ylamino)-1,2,3,4-tetrahydronaphthalen-2-yl]carbamic acid tert-butyl ester → N1-[5-(4-Trifluoromethylphenyl)oxazol-2-yl]-5,6,7,8-tetrahydronaphthalene-1,7-diamine

HRID 600811

反応式

HRID 600811 の反応式
C(OC(=O)[NH:7][CH:8]1[CH2:17][CH2:16][C:15]2[C:10](=[C:11]([NH:18][C:19]3[O:20][C:21]([C:24]4[CH:29]=[CH:28][C:27]([C:30]([F:33])([F:32])[F:31])=[CH:26][CH:25]=4)=[CH:22][N:23]=3)[CH:12]=[CH:13][CH:14]=2)[CH2:9]1)(C)(C)C.C(OC(=O)NC1CCC2C(=C(NC3OC(C4C=CC(C)=CC=4)=CN=3)C=CC=2)C1)(C)(C)C>>[F:33][C:30]([F:31])([F:32])[C:27]1[CH:28]=[CH:29][C:24]([C:21]2[O:20][C:19]([NH:18][C:11]3[C:10]4[CH2:9][CH:8]([NH2:7])[CH2:17][CH2:16][C:15]=4[CH:14]=[CH:13][CH:12]=3)=[N:23][CH:22]=2)=[CH:25][CH:26]=1

参加物

3

反応物 2

HCID 67229286[8-(5-p-Methylphenyloxazol-2-ylamino)-1,2,3,4-tetrahydronaphthalen-2-yl]carbamic acid tert-butyl esterHCID 67229897{8-[5-(4-Trifluoromethylphenyl)oxazol-2-ylamino]-1,2,3,4-tetrahydro-naphthalen-2-yl}carbamic acid tert-butyl ester

生成物 1

HCID 11964241N1-[5-(4-Trifluoromethylphenyl)oxazol-2-yl]-5,6,7,8-tetrahydronaphthalene-1,7-diamine収率 38.1%

実験手順

The title compound was prepared using the procedure as described in Example 20H substituting the product of Example 21A (120 mg, 0.253 mmol) for the product of Example 20G. The crude product was purified by trituration with Et2O/hexanes which resulted in 36 mg (38%) of the title compound as a white solid. 1H NMR (DMSO-d6) δ 9.32 (br s, 1H), 7.75 (m, 4H), 7.60 (s, 1H), 7.55 (d, J=7.8 Hz, 1H), 7.10 (t, J=7.8 Hz, 1H), 6.87 (d, J=7.8 Hz, 1H), 3.05-2.70 (m, 4H), 2.30 (m, 1H), 1.82 (m, 3H), 1.43 (m, 1H); MS (ESI+) m/z 374 (M+H)+.

後処理

  1. customThe title compound was prepared
  2. customThe crude product was purified by trituration with Et2O/hexanes which

出典と根拠

ORDレコード
ord-a5842a9ab4ca4f219143e6336acb443a
出典データセット
uspto-grants-2011_03
特許番号
US07902236B2

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