tert-Butyl (4-aminophenyl)carbamate → {4-[5-(6-Benzyloxy-naphthalen-2-yl)-pyrazolo[1,5-c]pyrimidin-7-ylamino]-phenyl}-carbamic acid tert-butyl ester

HRID 19608

反応式

HRID 19608 の反応式
[CH2:1]([O:8][C:9]1[CH:10]=[C:11]2[C:16](=[CH:17][CH:18]=1)[CH:15]=[C:14]([C:19]1[N:24]=[C:23](S(C)(=O)=O)[N:22]3[N:29]=[CH:30][CH:31]=[C:21]3[CH:20]=1)[CH:13]=[CH:12]2)[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1.[C:32]([O:36][C:37](=[O:46])[NH:38][C:39]1[CH:44]=[CH:43][C:42]([NH2:45])=[CH:41][CH:40]=1)([CH3:35])([CH3:34])[CH3:33]>>[C:32]([O:36][C:37](=[O:46])[NH:38][C:39]1[CH:40]=[CH:41][C:42]([NH:45][C:23]2[N:22]3[N:29]=[CH:30][CH:31]=[C:21]3[CH:20]=[C:19]([C:14]3[CH:13]=[CH:12][C:11]4[C:16](=[CH:17][CH:18]=[C:9]([O:8][CH2:1][C:2]5[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=5)[CH:10]=4)[CH:15]=3)[N:24]=2)=[CH:43][CH:44]=1)([CH3:35])([CH3:33])[CH3:34]

参加物

3

反応物 2

HCID 688611tert-Butyl (4-aminophenyl)carbamateHCID 673197765-(6-Benzyloxy-naphthalen-2-yl)-7-methanesulfonyl-pyrazolo[1,5-c]pyrimidine2 回

生成物 1

HCID 67319245{4-[5-(6-Benzyloxy-naphthalen-2-yl)-pyrazolo[1,5-c]pyrimidin-7-ylamino]-phenyl}-carbamic acid tert-butyl ester収率 46%

反応条件

温度
135 °C

実験手順

A mixture of 5-(6-benzyloxy-naphthalen-2-yl)-7-methanesulfonyl-pyrazolo[1,5-c]pyrimidine (compound D2)(87 mg) and 4-amino-phenyl-carbamic acid tert-butyl ester (208 mg) is heated neat at 130 to 140° C. bath temperature for 20 min. After cooling, the crude product is purified by silica gel flash chromatography. A nearly colorless solid (51 mg, 46%) with melting temperature of 189° C. is obtained.

後処理

  1. temperatureAfter cooling
  2. customthe crude product is purified by silica gel flash chromatography

出典と根拠

ORDレコード
ord-511010926b6f4983a5ba276bd9effa2d
出典データセット
uspto-grants-2010_06
特許番号
US07745446B2

関連ノート

読み込み中…