Ethyl isocyanate → (S)-ethyl-2-(4-(3-ethylureido)-3-fluorophenyl)-4-(3-methylmorpholino)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate

HRID 1626614ノート

反応式

HRID 1626614 の反応式
[NH2:1][C:2]1[CH:7]=[CH:6][C:5]([C:8]2[N:9]=[C:10]([N:22]3[CH2:27][CH2:26][O:25][CH2:24][C@@H:23]3[CH3:28])[C:11]3[CH2:16][N:15]([C:17]([O:19][CH2:20][CH3:21])=[O:18])[CH2:14][C:12]=3[N:13]=2)=[CH:4][C:3]=1[F:29].[CH2:30]([N:32]=[C:33]=[O:34])[CH3:31]>>[CH2:20]([O:19][C:17]([N:15]1[CH2:16][C:11]2[C:10]([N:22]3[CH2:27][CH2:26][O:25][CH2:24][C@@H:23]3[CH3:28])=[N:9][C:8]([C:5]3[CH:6]=[CH:7][C:2]([NH:1][C:33]([NH:32][CH2:30][CH3:31])=[O:34])=[C:3]([F:29])[CH:4]=3)=[N:13][C:12]=2[CH2:14]1)=[O:18])[CH3:21]

参加物

3

反応物 2

HCID 8022Ethyl isocyanateHCID 66679065(S)-ethyl 2-(4-amino-3-fluorophenyl)-4-(3-methylmorpholino)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate2 回

生成物 1

HCID 66679183(S)-ethyl-2-(4-(3-ethylureido)-3-fluorophenyl)-4-(3-methylmorpholino)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate収率 22%

実験手順

Method as described for example 85 using (S)-ethyl 2-(4-amino-3-fluorophenyl)-4-(3-methylmorpholino)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (intermediate 19) and ethyl isocyanate as starting materials. The solvent was removed in vacuo and the residue purified by prep HPLC (high pH) yielding the title compound (10 mg, 0.021 mmol, 22%).

後処理

  1. customThe solvent was removed in vacuo
  2. customthe residue purified by prep HPLC (high pH)

出典と根拠

ORDレコード
ord-06d8c94e422d4a72a249851394fc32a1
出典データセット
uspto-grants-2014_07
特許番号
US08785457B2

反応ノート

読み込み中…