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

HRID 74229노트

반응식

HRID 74229 반응식
[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

참가 물질

4

반응물 2

HCID 15050Trimethyl orthoacetateHCID 67498091HCID 67498091, 화합물

생성물 1

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

시약·촉매·용매 1

HCID 887Methanol용매

실험 절차

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.

후처리

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

출처 및 근거

ORD 기록
ord-34159f691ed3462a99625c552f00d970
출처 데이터셋
uspto-grants-2014_09
특허 번호
US08829035B2

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