Diisopropylethylamine → HCID 73053060、化合物

HRID 2275496ノート

反応式

HRID 2275496 の反応式
[O:1]=[C:2]1[NH:6][CH:5]=[C:4]([C:7]([OH:9])=O)[O:3]1.CN(C(ON1N=NC2C=CC=NC1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F.[NH2:34][C@H:35]([CH2:44][C:45]1[CH:50]=[CH:49][C:48]([C:51]2[CH:56]=[C:55]([Cl:57])[CH:54]=[CH:53][C:52]=2[F:58])=[CH:47][CH:46]=1)[CH2:36][C@:37]([CH2:42][OH:43])([CH3:41])[C:38]([OH:40])=[O:39].CCN(C(C)C)C(C)C>CN(C=O)C>[Cl:57][C:55]1[CH:54]=[CH:53][C:52]([F:58])=[C:51]([C:48]2[CH:47]=[CH:46][C:45]([CH2:44][C@@H:35]([NH:34][C:7]([C:4]3[O:3][C:2](=[O:1])[NH:6][CH:5]=3)=[O:9])[CH2:36][C@:37]([CH2:42][OH:43])([CH3:41])[C:38]([OH:40])=[O:39])=[CH:50][CH:49]=2)[CH:56]=1

参加物

6

反応物 4

HCID 81531DiisopropylethylamineHCID 9886157Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)HCID 539814232-Hydroxy-1,3-oxazole-5-carboxylic acidHCID 89964351HCID 89964351、化合物

生成物 1

HCID 73053060HCID 73053060、化合物収率 11.4%

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒2 回

実験手順

2-Oxo-2,3-dihydrooxazole-5-carboxylic acid (7.1 mg, 55 μmol) and HATU (21 mg, 55 μmol) were combined in DMF (0.3 mL) and stirred at room temperature for 5 minutes. (2S,4R)-4-Amino-5-(5′-chloro-2′-fluorobiphenyl-4-yl)-2-hydroxymethyl-2-methylpentanoic acid (20 mg, 55 μmol) in DMF (0.5 mL) and DIPEA (29 μL, 164 μmol) were added, and the resulting mixture was stirred for 10 minutes at room temperature. The mixture was concentrated under reduced pressure and the residue was dissolved in AcOH purified by preparative HPLC to yield the title compound (3 mg). MS m/z [M+H]+ calc'd for C23H22ClFN2O6, 477.12. found 477.

後処理

  1. stirringthe resulting mixture was stirred for 10 minutes at room temperature
  2. concentrationThe mixture was concentrated under reduced pressure
  3. dissolutionthe residue was dissolved in AcOH
  4. custompurified by preparative HPLC

出典と根拠

ORDレコード
ord-10941a0ca6c7409d8e18ff8071ca324a
出典データセット
uspto-grants-2015_09
特許番号
US09126956B2

反応ノート

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