2-Dimethylaminopyridine → Morpholine-4-carboxylic acid 2-[6-(4-tert-butyl-phenylsulfonylamino)-5-(3-methoxy-phenoxy)-pyrimidin-4-yloxy]-ethyl ester

HRID 1736393

반응식

HRID 1736393 반응식
[N:1]1([C:7](Cl)=[O:8])[CH2:6][CH2:5][O:4][CH2:3][CH2:2]1.[C:10]([C:14]1[CH:19]=[CH:18][C:17]([S:20]([NH:23][C:24]2[C:29]([O:30][C:31]3[CH:36]=[CH:35][CH:34]=[C:33]([O:37][CH3:38])[CH:32]=3)=[C:28]([O:39][CH2:40][CH2:41][OH:42])[N:27]=[CH:26][N:25]=2)(=[O:22])=[O:21])=[CH:16][CH:15]=1)([CH3:13])([CH3:12])[CH3:11].CN(C1C=CC=CN=1)C>>[C:10]([C:14]1[CH:15]=[CH:16][C:17]([S:20]([NH:23][C:24]2[N:25]=[CH:26][N:27]=[C:28]([O:39][CH2:40][CH2:41][O:42][C:7]([N:1]3[CH2:6][CH2:5][O:4][CH2:3][CH2:2]3)=[O:8])[C:29]=2[O:30][C:31]2[CH:36]=[CH:35][CH:34]=[C:33]([O:37][CH3:38])[CH:32]=2)(=[O:22])=[O:21])=[CH:18][CH:19]=1)([CH3:13])([CH3:11])[CH3:12]

참가 물질

4

반응물 3

HCID 218852-DimethylaminopyridineHCID 848104-Morpholinecarbonyl chlorideHCID 122044Ro 46-2005

생성물 1

HCID 54072965Morpholine-4-carboxylic acid 2-[6-(4-tert-butyl-phenylsulfonylamino)-5-(3-methoxy-phenoxy)-pyrimidin-4-yloxy]-ethyl ester

실험 절차

In analogy to Example 1, part a), from 0.15 ml of morpholine-4-carbonyl chloride and 200 mg of p-tert-butyl-N-[6-(2-hydroxy-ethoxy) -5-(m-methoxyphenoxy)-4-pyrimidinyl]benzenesulfonamide with the addition of 154 mg of dimethylaminopyridine at a reaction period of 12 hours there was obtained morpholine-4-carboxylic acid 2-[6-(4-tert -butyl-phenylsulfonylamino)-5-(3-methoxy-phenoxy)-pyrimidin-4-yloxy]-ethyl ester. MS: 587.4 (M+H).

후처리

  1. customat a reaction period of 12 hours there

출처 및 근거

ORD 기록
ord-b54aaf3a09f043688c195c0eb7a46914
출처 데이터셋
uspto-grants-1996_07
특허 번호
US05541186

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