1-Hydroxybenzotriazole → 4-[4-[4-(cis-2,6-Dimethylmorpholin-4-yl)phenyl]piperazin-1-yl]benzoic acid benzotriazol-1-yl ester

HRID 1816754노트

반응식

HRID 1816754 반응식
[CH3:1][C@H:2]1[O:7][C@@H:6]([CH3:8])[CH2:5][N:4]([C:9]2[CH:14]=[CH:13][C:12]([N:15]3[CH2:20][CH2:19][N:18]([C:21]4[CH:29]=[CH:28][C:24]([C:25]([OH:27])=[O:26])=[CH:23][CH:22]=4)[CH2:17][CH2:16]3)=[CH:11][CH:10]=2)[CH2:3]1.O[N:31]1[C:35]2[CH:36]=[CH:37][CH:38]=[CH:39][C:34]=2[N:33]=[N:32]1.Cl.C(N=C=NCCCN(C)C)C>C(Cl)Cl>[N:31]1([O:26][C:25](=[O:27])[C:24]2[CH:28]=[CH:29][C:21]([N:18]3[CH2:17][CH2:16][N:15]([C:12]4[CH:11]=[CH:10][C:9]([N:4]5[CH2:5][C@H:6]([CH3:8])[O:7][C@H:2]([CH3:1])[CH2:3]5)=[CH:14][CH:13]=4)[CH2:20][CH2:19]3)=[CH:22][CH:23]=2)[C:35]2[CH:36]=[CH:37][CH:38]=[CH:39][C:34]=2[N:33]=[N:32]1

참가 물질

5

반응물 3

HCID 757711-HydroxybenzotriazoleHCID 27239391,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochlorideHCID 543123714-[4-[4-(cis-2,6-Dimethylmorpholin-4-yl)phenyl]piperazin-1-yl]benzoic acid

생성물 1

HCID 540341114-[4-[4-(cis-2,6-Dimethylmorpholin-4-yl)phenyl]piperazin-1-yl]benzoic acid benzotriazol-1-yl ester수율 91.4%

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

A mixture of 4-[4-[4-(cis-2,6-dimethylmorpholin-4-yl)phenyl]piperazin-1-yl]benzoic acid (1.01 g), 1-hydroxybenzotriazole (370 mg) and 1-ethyl-3-(3′-dimethylaminopropyl)carbodiimide hydrochloride (986 mg) in methylene chloride (100 ml) was stirred for 4 hours at room temperature then evaporated under reduced pressure. Water was added to the residue and the resulting precipitate collected by filtration, washed with water, then dried under hi-vacuum to give 4-[4-[4-(cis-2,6-dimethylmorpholin-4-yl)phenyl]piperazin-1-yl]benzoic acid benzotriazol-1-yl ester (1.197 g).

후처리

  1. customthen evaporated under reduced pressure
  2. additionWater was added to the residue
  3. filtrationthe resulting precipitate collected by filtration
  4. washwashed with water
  5. customdried under hi-vacuum

출처 및 근거

ORD 기록
ord-b8c42fa33ebf4e488bd92073a15556a7
출처 데이터셋
uspto-grants-2005_04
특허 번호
US06884868B1

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