Phenylacetic Acid → N-cyclopropyl-6-methyl-4'-(5-{[(phenylacetyl)amino]methyl}-1,3,4-oxadiazol-2-yl)-1,1'-biphenyl-3-carboxamide

HRID 31489

反応式

HRID 31489 の反応式
[C:1]1([CH2:7][C:8]([OH:10])=O)[CH:6]=[CH:5][CH:4]=[CH:3][CH:2]=1.CN(C(ON1N=NC2C=CC=NC1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F.C1C=CC2N(O)N=NC=2C=1.CCN(C(C)C)C(C)C.[NH2:54][CH2:55][C:56]1[O:60][C:59]([C:61]2[CH:66]=[CH:65][C:64]([C:67]3[C:72]([CH3:73])=[CH:71][CH:70]=[C:69]([C:74]([NH:76][CH:77]4[CH2:79][CH2:78]4)=[O:75])[CH:68]=3)=[CH:63][CH:62]=2)=[N:58][N:57]=1>CN(C=O)C>[CH:77]1([NH:76][C:74]([C:69]2[CH:68]=[C:67]([C:64]3[CH:65]=[CH:66][C:61]([C:59]4[O:60][C:56]([CH2:55][NH:54][C:8](=[O:10])[CH2:7][C:1]5[CH:2]=[CH:3][CH:4]=[CH:5][CH:6]=5)=[N:57][N:58]=4)=[CH:62][CH:63]=3)[C:72]([CH3:73])=[CH:71][CH:70]=2)=[O:75])[CH2:79][CH2:78]1

参加物

7

反応物 5

HCID 999Phenylacetic AcidHCID 757711-HydroxybenzotriazoleHCID 81531DiisopropylethylamineHCID 9886157Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)HCID 99978914'-[5-(aminomethyl)-1,3,4-oxadiazol-2-yl]-N-cyclopropyl-6-methyl-1,1'-biphenyl-3-carboxamide

生成物 1

HCID 10434691N-cyclopropyl-6-methyl-4'-(5-{[(phenylacetyl)amino]methyl}-1,3,4-oxadiazol-2-yl)-1,1'-biphenyl-3-carboxamide

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒2 回

実験手順

Phenylacetic acid (12 mg) and HATU (33 mg) in DMF (1 ml) were stirred for 10 minutes at room temperature. To this solution was added HOBt (11.6 mg), DIPEA (.0.45 ml) and 4′-[5-(aminomethyl)-1,3,4-oxadiazol-2-yl]-N-cyclopropyl-6-methyl-1,1′-biphenyl-3-carboxamide (Example 53) (30 mg) in DMF (2 ml) and the reaction stirred at room temperature for 18 hours. The solvent was evaporated under vacuum and the residue dissolved in DMSO (0.25 ml), methanol (0.25 ml) was added and the precipitate produced isolated by filtration to give N-cyclopropyl-6-methyl-4′-(5-{[(phenylacetyl)amino]methyl}-1,3,4-oxadiazol-2-yl)-1,1′-biphenyl-3-carboxamide.

後処理

  1. customThe solvent was evaporated under vacuum
  2. dissolutionthe residue dissolved in DMSO (0.25 ml)
  3. additionmethanol (0.25 ml) was added
  4. customthe precipitate produced
  5. customisolated by filtration

出典と根拠

ORDレコード
ord-952287615a4c4aa1a2e947ff07f4271d
出典データセット
uspto-grants-2008_09
特許番号
US07425555B2

関連ノート

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