Norchlorcyclizine → Cetirizine ethyl ester

HRID 1871010노트

반응식

HRID 1871010 반응식
[Cl:1][C:2]1[CH:7]=[CH:6][C:5]([CH:8]([C:15]2[CH:20]=[CH:19][CH:18]=[CH:17][CH:16]=2)[N:9]2[CH2:14][CH2:13][NH:12][CH2:11][CH2:10]2)=[CH:4][CH:3]=1.Cl[CH2:22][CH2:23][O:24][CH2:25][C:26]([O:28][CH2:29][CH3:30])=[O:27]>[I-].C([N+](CCCC)(CCCC)CCCC)CCC.C(N(CC)CC)C>[Cl:1][C:2]1[CH:3]=[CH:4][C:5]([CH:8]([C:15]2[CH:16]=[CH:17][CH:18]=[CH:19][CH:20]=2)[N:9]2[CH2:10][CH2:11][N:12]([CH2:22][CH2:23][O:24][CH2:25][C:26]([O:28][CH2:29][CH3:30])=[O:27])[CH2:13][CH2:14]2)=[CH:6][CH:7]=1

참가 물질

5

반응물 2

HCID 9340NorchlorcyclizineHCID 10964894Ethyl 2-(2-chloroethoxy)acetate

생성물 1

HCID 9844843Cetirizine ethyl ester수율 90.8%

시약·촉매·용매 2

HCID 67553Tetrabutylammonium Iodide촉매HCID 8471Triethylamine용매

실험 절차

10 gr. (0.035 mole) of 1-[(4-chlorophenyl)phenylmethyl]piperazine, 8.8 gr. of ethyl 2-chloroethoxyacetate, 0.4. gr. of tetrabutylammonium iodide and 50 ml. of triethylamine were introduced into a pressure vessel and treated as described in example 1. 13.2 gr. of ethyl [2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetate is obtained (90.8% yield).

후처리

  1. additiontreated

출처 및 근거

ORD 기록
ord-77086cb68edd41a7bb03b3a213a00040
출처 데이터셋
uspto-grants-2000_08
특허 번호
US06100400

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