2-(Methylthio)thiazolo[5,4-b]pyridine → 1-acetyl-N-(thiazolo[5,4-b]pyridin-2-yl)-4-piperidinemethanamine

HRID 1789494

反応式

HRID 1789494 の反応式
[C:1]([N:4]1[CH2:9][CH2:8][CH:7]([CH2:10][NH2:11])[CH2:6][CH2:5]1)(=[O:3])[CH3:2].CS[C:14]1[S:15][C:16]2[C:21]([N:22]=1)=[CH:20][CH:19]=[CH:18][N:17]=2>>[C:1]([N:4]1[CH2:5][CH2:6][CH:7]([CH2:10][NH:11][C:14]2[S:15][C:16]3[C:21]([N:22]=2)=[CH:20][CH:19]=[CH:18][N:17]=3)[CH2:8][CH2:9]1)(=[O:3])[CH3:2]

参加物

3

反応物 2

HCID 6998402-(Methylthio)thiazolo[5,4-b]pyridineHCID 126870221-(4-(Aminomethyl)piperidin-1-yl)ethan-1-one

生成物 1

HCID 212415751-acetyl-N-(thiazolo[5,4-b]pyridin-2-yl)-4-piperidinemethanamine収率 93%

反応条件

温度
140 °C

実験手順

A mixture of 11 parts of 1-acetyl-4-piperidinemethanamine and 9 parts of 2-(methylthio)thiazolo[5,4-b]pyridine was stirred and heated for 20 hours at 140° C. The whole was purified by column chromatography over silica gel using a mixture of trichloromethane and methanol (95:5 by volume) as eluent. The pure fractions were collected and the eluent was evaporated, yielding 13.5 parts (93%) of 1-acetyl-N-(thiazolo[5,4-b]pyridin-2-yl)-4-piperidinemethanamine as a residue (intermediate 51).

後処理

  1. customThe whole was purified by column chromatography over silica gel using
  2. additiona mixture of trichloromethane and methanol (95:5 by volume) as eluent
  3. customThe pure fractions were collected
  4. customthe eluent was evaporated

出典と根拠

ORDレコード
ord-9e71969e97bc4104b9560ff69314f6e6
出典データセット
uspto-grants-1987_08
特許番号
US04689330

関連ノート

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