1-Aminoindane, (S)- → HCID 66797896、化合物

HRID 447582ノート

反応式

HRID 447582 の反応式
Cl[C:2]1[N:7]=[CH:6][N:5]=[C:4]([NH:8][C@H:9]2[CH2:13][C@H:12]([OH:14])[C@@H:11]([CH2:15][OH:16])[CH2:10]2)[CH:3]=1.[NH2:17][C@@H:18]1[C:26]2[C:21](=[CH:22][CH:23]=[CH:24][CH:25]=2)[CH2:20][CH2:19]1>C(O)CCC>[C@@H:18]1([NH:17][C:2]2[N:7]=[CH:6][N:5]=[C:4]([NH:8][C@H:9]3[CH2:13][C@H:12]([OH:14])[C@@H:11]([CH2:15][OH:16])[CH2:10]3)[CH:3]=2)[C:26]2[C:21](=[CH:22][CH:23]=[CH:24][CH:25]=2)[CH2:20][CH2:19]1

参加物

4

反応物 2

HCID 70000841-Aminoindane, (S)-HCID 59671414HCID 59671414、化合物

生成物 1

HCID 66797896HCID 66797896、化合物収率 73.5%

試薬・触媒・溶媒 1

HCID 2631-Butanol溶媒

反応条件

温度
200 °C

実験手順

A mixture of (1S,2R,4R)-4-[(6-chloropyrimidin-4-yl)amino]-2-(hydroxymethyl)cyclopentanol (500. mg, 2.05 mmol), 1-butanol (4.00 mL) and (S)-(+)-1-aminoindan (0.806 mL, 6.16 mmol) was heated to 200° C. for 90 min in a sealed tube using MWI. The mixture was concentrated in vacuo and purified via silica gel chromatography eluting with a gradient of 5 to 25% MeOH in DCM to afford the title compound as an amorphous solid (513 mg, 73%). LC/MS: Rt=1.20 min, ES+ 341 (AA standard).

後処理

  1. concentrationThe mixture was concentrated in vacuo
  2. custompurified via silica gel chromatography
  3. washeluting with a gradient of 5 to 25% MeOH in DCM

出典と根拠

ORDレコード
ord-26063974e63d41be8defa7f186face64
出典データセット
uspto-grants-2013_07
特許番号
US08481550B2

反応ノート

読み込み中…