Ammonia → AZD7118 Bromo Amide

HRID 2061844노트

반응식

HRID 2061844 반응식
[Br:1][C:2]1[C:7]([C:8](OC)=[O:9])=[CH:6][C:5]([NH:12][C:13]([NH:15][CH2:16][CH3:17])=[O:14])=[N:4][CH:3]=1.[NH3:18]>CO>[Br:1][C:2]1[C:7]([C:8]([NH2:18])=[O:9])=[CH:6][C:5]([NH:12][C:13]([NH:15][CH2:16][CH3:17])=[O:14])=[N:4][CH:3]=1

참가 물질

4

반응물 2

HCID 222AmmoniaHCID 59416007Methyl 5-bromo-2-(3-ethylureido)isonicotinate2회

생성물 1

HCID 59208425AZD7118 Bromo Amide수율 95.1%

시약·촉매·용매 1

HCID 887Methanol용매

실험 절차

A solution of methyl 5-bromo-2-(3-ethylureido)isonicotinate (Intermediate 1, 56.22 g, 186.0 mmol) in 7N ammonia in methanol (1 L) was allowed to stir at room temperature in a sealed flask for 1½ d. The precipitate that formed was collected by filtration, rinsed with acetonitrile (500 mL), and then dried on the high vacuum pump overnight, yielding 50.8 g of a solid (95.1%).

후처리

  1. customThe precipitate that formed
  2. filtrationwas collected by filtration
  3. washrinsed with acetonitrile (500 mL)
  4. customdried on the high vacuum pump overnight

출처 및 근거

ORD 기록
ord-332ea4bf248e4bceb9b805eb835e8b83
출처 데이터셋
uspto-grants-2012_10
특허 번호
US08283361B2

반응 노트

불러오는 중…