Trifluoroacetic acid → HCID 58183109、化合物

HRID 1469411ノート

反応式

HRID 1469411 の反応式
[F:1][C:2]([F:52])([F:51])[C:3]1[CH:4]=[C:5]([C:13]([CH3:50])([CH3:49])[C:14]([N:16]([CH3:48])[C:17]2[C:18]([C:40]3[CH:45]=[CH:44][C:43]([F:46])=[CH:42][C:41]=3[CH3:47])=[CH:19][C:20]([C@H:23]3[N:27](C(OC(C)(C)C)=O)[C@@:26]([CH3:39])([C:35]([O:37][CH3:38])=[O:36])[CH2:25][CH2:24]3)=[N:21][CH:22]=2)=[O:15])[CH:6]=[C:7]([C:9]([F:12])([F:11])[F:10])[CH:8]=1.C(O)(C(F)(F)F)=O>ClCCl>[F:52][C:2]([F:1])([F:51])[C:3]1[CH:4]=[C:5]([C:13]([CH3:49])([CH3:50])[C:14]([N:16]([CH3:48])[C:17]2[C:18]([C:40]3[CH:45]=[CH:44][C:43]([F:46])=[CH:42][C:41]=3[CH3:47])=[CH:19][C:20]([C@H:23]3[NH:27][C@@:26]([CH3:39])([C:35]([O:37][CH3:38])=[O:36])[CH2:25][CH2:24]3)=[N:21][CH:22]=2)=[O:15])[CH:6]=[C:7]([C:9]([F:11])([F:12])[F:10])[CH:8]=1

参加物

4

反応物 2

HCID 6422Trifluoroacetic acidHCID 579655771-(1,1-dimethylethyl) 2-methyl (2R,5S)-5-[5-[{2-[3,5-bis(trifluoromethyl)phenyl]-2-methylpropanoyl}(methyl)amino]-4-(4-fluoro-2-methylphenyl)-2-pyridinyl]-2-methyl-1,2-pyrrolidinedicarboxylate2 回

生成物 1

HCID 58183109HCID 58183109、化合物収率 91%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

To a solution of 1-(1,1-dimethylethyl) 2-methyl (2R,5S)-5-[5-[{2-[3,5-bis(trifluoromethyl)phenyl]-2-methylpropanoyl}(methyl)amino]-4-(4-fluoro-2-methylphenyl)-2-pyridinyl]-2-methyl-1,2-pyrrolidinedicarboxylate (Intermediate 19, 70 mg, 0.095 mmol) in dry Dichloromethane (DCM) (2 ml) was added TFA (0.5 ml, 6.49 mmol) and the reaction mixture was stirred for 2.5 hours at r.t. The solvent and the excess of TFA were evaporated and the residue was purified by SPE-SCX cartridge to afford the title compound (55 mg, 0.086 mmol, 91% yield) as a white solid. UPLC: Rt 0.76 min (broad peak), m/z 640 [M+H]+.

後処理

  1. customThe solvent and the excess of TFA were evaporated
  2. customthe residue was purified by SPE-SCX cartridge

出典と根拠

ORDレコード
ord-074c36d84fe848fbbf28f363590d3613
出典データセット
uspto-grants-2015_04
特許番号
US09006271B2

反応ノート

読み込み中…