Trimethyl orthoacetate → 5-(Benzoxazol-2-yl)-2-methyl-1-cyclopropylmethylbenzimidazole

HRID 74229ノート

反応式

HRID 74229 の反応式
[CH:1]1([CH2:4][NH:5][C:6]2[CH:12]=[CH:11][C:10]([C:13]3[O:14][C:15]4[CH:21]=[CH:20][CH:19]=[CH:18][C:16]=4[N:17]=3)=[CH:9][C:7]=2[NH2:8])[CH2:3][CH2:2]1.CO[C:24](OC)(OC)[CH3:25]>CO>[O:14]1[C:15]2[CH:21]=[CH:20][CH:19]=[CH:18][C:16]=2[N:17]=[C:13]1[C:10]1[CH:11]=[CH:12][C:6]2[N:5]([CH2:4][CH:1]3[CH2:2][CH2:3]3)[C:24]([CH3:25])=[N:8][C:7]=2[CH:9]=1

参加物

4

反応物 2

HCID 15050Trimethyl orthoacetateHCID 67498091HCID 67498091、化合物

生成物 1

HCID 674980925-(Benzoxazol-2-yl)-2-methyl-1-cyclopropylmethylbenzimidazole収率 63.5%

試薬・触媒・溶媒 1

HCID 887Methanol溶媒

実験手順

To a methanol (5 mL) solution of 2-(2-cyclopropylmethylaminoanilin-5-yl)benzoxazole (see Working Example 54-1) (140 mg, 0.425 mmol) was added 1,1,1-trimethoxyethane (75 mg, 0.624 mmol), and this was stirred at room temperature for 10 hours. After the reaction was complete, this was concentrated, and the residue obtained was purified by silica gel column chromatography to yield the title compound (81.9 mg, 54% yield) as pink crystals.

後処理

  1. concentrationthis was concentrated
  2. customthe residue obtained
  3. customwas purified by silica gel column chromatography

出典と根拠

ORDレコード
ord-34159f691ed3462a99625c552f00d970
出典データセット
uspto-grants-2014_09
特許番号
US08829035B2

反応ノート

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