Water → 5-{7-(2-chloro-4-pyridyl)-8-(3-(trifluoromethyl)phenyl)-1,2,4-triazolo[4,3-c]pyrimidin-5-yl}-2-(tert-butoxycarbonyl)-(1R)-2,5-diaza-bicyclo[2.2.1]heptane

HRID 897404ノート

反応式

HRID 897404 の反応式
Cl[C:2]1[N:7]2[CH:8]=[N:9][N:10]=[C:6]2[C:5]([C:11]2[CH:16]=[CH:15][CH:14]=[C:13]([C:17]([F:20])([F:19])[F:18])[CH:12]=2)=[C:4]([C:21]2[CH:26]=[CH:25][N:24]=[C:23]([Cl:27])[CH:22]=2)[N:3]=1.C(=O)([O-])[O-].[K+].[K+].[C:34]([O:38][C:39]([N:41]1[CH2:46][C@H:45]2[CH2:47][C@@H:42]1[CH2:43][NH:44]2)=[O:40])([CH3:37])([CH3:36])[CH3:35].O>CN(C=O)C>[Cl:27][C:23]1[CH:22]=[C:21]([C:4]2[N:3]=[C:2]([N:44]3[CH2:43][C@H:42]4[CH2:47][CH:45]3[CH2:46][N:41]4[C:39]([O:38][C:34]([CH3:37])([CH3:36])[CH3:35])=[O:40])[N:7]3[CH:8]=[N:9][N:10]=[C:6]3[C:5]=2[C:11]2[CH:16]=[CH:15][CH:14]=[C:13]([C:17]([F:18])([F:20])[F:19])[CH:12]=2)[CH:26]=[CH:25][N:24]=1

参加物

6

反応物 4

HCID 962WaterHCID 11430Potassium CarbonateHCID 11860399N-Boc-2,5-diazabicyclo[2.2.1]heptaneHCID 223466035-Chloro-7-(2-chloro-4-pyridyl)-8-(3-(trifluoromethyl)phenyl)-1,2,4-triazolo[4,3-c]pyrimidine

生成物 1

HCID 208169155-{7-(2-chloro-4-pyridyl)-8-(3-(trifluoromethyl)phenyl)-1,2,4-triazolo[4,3-c]pyrimidin-5-yl}-2-(tert-butoxycarbonyl)-(1R)-2,5-diaza-bicyclo[2.2.1]heptane

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

A mixture of 5-chloro-7-(2-chloro-4-pyridyl)-8-(3-(trifluoromethyl)-phenyl)-1,2,4-triazolo[4,3-c]pyrimidine (820 mg, 2.0 mmole), potassium carbonate (ca. 1.0 g) and (−)-2-(tert-butoxycarbonyl)-(1R, 4R)-2,5-diaza-bicyclo[2.2.1]heptane (436 mg, 2.2 mmole) in 10 ml of DMF was stirred at room temperature for 16 hours. The reaction solution was poured into water (50 mL), and precipitate was filtered and washed with water and dried under vacuum to give product as off white solid; MS m/z (M)+ 572.3; C27H25ClF3N7O2 requir. 572.

後処理

  1. filtrationwas filtered
  2. washwashed with water
  3. customdried under vacuum
  4. customto give product as off white solid

出典と根拠

ORDレコード
ord-3eceb919491a46659ec43915b1b11fbf
出典データセット
uspto-grants-2005_07
特許番号
US06921762B2

反応ノート

読み込み中…