Tetrahydrofuran → 2-[4-(2-{4-{{Di(tert-butoxy)phosphoryl](difluoro)methyl]benzyl}-3-oxo-2,3-diphenylpropyl)phenyl]-2,2-difluoroacetic acid

HRID 566515ノート

反応式

HRID 566515 の反応式
[F:1][C:2]([F:46])([P:42]([OH:45])(O)=[O:43])[C:3]1[CH:41]=[CH:40][C:6]([CH2:7][C:8]([C:32]2[CH:37]=[CH:36][C:35](SC)=[CH:34][CH:33]=2)([C:23]([C:25]2[CH:30]=[CH:29][CH:28]=[C:27](F)[CH:26]=2)=[O:24])[CH2:9][C:10]2[CH:15]=[CH:14][C:13](OP(C(F)F)(=O)O)=[CH:12][CH:11]=2)=[CH:5][CH:4]=1.[CH2:47]1OCCOCCOCCOCCOCCOC1.[CH3:65][C:66]([CH3:69])([O-:68])[CH3:67].[K+].BrCC1C=CC([C:79]([F:88])([F:87])[C:80]([O:82]C(C)(C)C)=[O:81])=CC=1.[CH2:89]1[CH2:93]OC[CH2:90]1>[N+](CCCC)(CCCC)(CCCC)CCCC.[I-]>[C:66]([O:68][P:42]([C:2]([F:1])([F:46])[C:3]1[CH:41]=[CH:40][C:6]([CH2:7][C:8]([C:32]2[CH:37]=[CH:36][CH:35]=[CH:34][CH:33]=2)([C:23](=[O:24])[C:25]2[CH:26]=[CH:27][CH:28]=[CH:29][CH:30]=2)[CH2:9][C:10]2[CH:15]=[CH:14][C:13]([C:79]([F:88])([F:87])[C:80]([OH:82])=[O:81])=[CH:12][CH:11]=2)=[CH:5][CH:4]=1)([O:45][C:89]([CH3:90])([CH3:93])[CH3:47])=[O:43])([CH3:69])([CH3:67])[CH3:65]

参加物

7

反応物 5

HCID 8028Tetrahydrofuran2 回HCID 2855718-Crown-6HCID 14888669HCID 14888669、化合物HCID 23665647Potassium tert-butoxideHCID 88067715HCID 88067715、化合物

生成物 1

HCID 212657102-[4-(2-{4-{{Di(tert-butoxy)phosphoryl](difluoro)methyl]benzyl}-3-oxo-2,3-diphenylpropyl)phenyl]-2,2-difluoroacetic acid

試薬・触媒・溶媒 1

HCID 67553Tetrabutylammonium Iodide触媒

実験手順

To the compound of Example 33 (0.100 g, 0.189 mmol) in THF (0.90 mL) were added nBu4NI (catalytic) and a trace of 18-crown-6. To this mixture at −78° C. was added potassium tert-butoxide (1M in THF, 0.208 mL) after a period of 10 min at −78° C., a THF solution (0.30 mL) of tert-butyl 2-[4-(bromomethyl)phenyl]-2,2-difluoroacetate](0.066 g, 0.206 mmol) was added. After a period of 2 h, at 0° C., the reaction mixture was quenched as described for Example 31 Step 1.

後処理

  1. customat 0° C., the reaction mixture was quenched

出典と根拠

ORDレコード
ord-4d010512c9ed495d9b6d46dbf2a5252a
出典データセット
uspto-grants-2001_01
特許番号
US06174874B1

反応ノート

読み込み中…