4-[2-(N-Boc-N-methylamino)ethyl]benzoic acid → tert-Butyl (2-{4-[{3-[({[(2S)-1'-{2-[(5R)-3-[3,5-bis(trifluoromethyl)benzoyl]-5-(4-fluorophenyl)-1,3-oxazolidin-5-yl]ethyl}-2,3-dihydrospiro[indene-1,4'-piperidin]-2-yl]oxy}acetyl)(methyl)amino]propyl}(methyl)carbamoyl]phenyl}ethyl)methylcarbamate

HRID 446544ノート

反応式

HRID 446544 の反応式
[C:1]([O:5][C:6]([N:8]([CH3:20])[CH2:9][CH2:10][C:11]1[CH:19]=[CH:18][C:14]([C:15]([OH:17])=O)=[CH:13][CH:12]=1)=[O:7])([CH3:4])([CH3:3])[CH3:2].[F:21][C:22]([F:75])([F:74])[C:23]1[CH:24]=[C:25]([CH:67]=[C:68]([C:70]([F:73])([F:72])[F:71])[CH:69]=1)[C:26]([N:28]1[CH2:32][C@@:31]([CH2:40][CH2:41][N:42]2[CH2:47][CH2:46][C:45]3([C:55]4[C:50](=[CH:51][CH:52]=[CH:53][CH:54]=4)[CH2:49][C@@H:48]3[O:56][CH2:57][C:58]([N:60]([CH3:66])[CH2:61][CH2:62][CH2:63][NH:64][CH3:65])=[O:59])[CH2:44][CH2:43]2)([C:33]2[CH:38]=[CH:37][C:36]([F:39])=[CH:35][CH:34]=2)[O:30][CH2:29]1)=[O:27]>>[F:73][C:70]([F:71])([F:72])[C:68]1[CH:67]=[C:25]([CH:24]=[C:23]([C:22]([F:21])([F:75])[F:74])[CH:69]=1)[C:26]([N:28]1[CH2:32][C@@:31]([CH2:40][CH2:41][N:42]2[CH2:43][CH2:44][C:45]3([C:55]4[C:50](=[CH:51][CH:52]=[CH:53][CH:54]=4)[CH2:49][C@@H:48]3[O:56][CH2:57][C:58]([N:60]([CH3:66])[CH2:61][CH2:62][CH2:63][N:64]([CH3:65])[C:15]([C:14]3[CH:13]=[CH:12][C:11]([CH2:10][CH2:9][N:8]([CH3:20])[C:6](=[O:7])[O:5][C:1]([CH3:2])([CH3:3])[CH3:4])=[CH:19][CH:18]=3)=[O:17])=[O:59])[CH2:46][CH2:47]2)([C:33]2[CH:34]=[CH:35][C:36]([F:39])=[CH:37][CH:38]=2)[O:30][CH2:29]1)=[O:27]

参加物

3

反応物 2

HCID 666713624-[2-(N-Boc-N-methylamino)ethyl]benzoic acidHCID 866634192-{[(2S)-1'-{2-[(5R)-3-[3,5-Bis(trifluoromethyl)benzoyl]-5-(4-fluorophenyl)-1,3-oxazolidin-5-yl]ethyl}-2,3-dihydrospiro[indene-1,4'-piperidin]-2-yl]oxy}-N-methyl-N-[3-(methylamino)propyl]acetamide

生成物 1

HCID 86663448tert-Butyl (2-{4-[{3-[({[(2S)-1'-{2-[(5R)-3-[3,5-bis(trifluoromethyl)benzoyl]-5-(4-fluorophenyl)-1,3-oxazolidin-5-yl]ethyl}-2,3-dihydrospiro[indene-1,4'-piperidin]-2-yl]oxy}acetyl)(methyl)amino]propyl}(methyl)carbamoyl]phenyl}ethyl)methylcarbamate収率 92%

実験手順

The compound (140 mg, 0.501 mmol) obtained in Example 50a and the compound (260 mg, 334 mol) obtained in Example 1k were used to give the title compound (320 mg; yield, 92%) as a white solid according to the method described in Example 41a.

出典と根拠

ORDレコード
ord-bbcea42410404bcd815290b0d54aadce
出典データセット
uspto-grants-2013_07
特許番号
US08476253B2

反応ノート

読み込み中…