N-(2,2-dimethoxyethyl)-N-(4-fluorobenzyl)amine → 2-(3-(2,2-dimethoxyethyl)-3-(4-fluorobenzyl)ureido)-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide

HRID 560538노트

반응식

HRID 560538 반응식
[CH3:1][O:2]C(OC)CNC1C=CC(F)=CC=1.[F:15][C:16]1[CH:29]=[CH:28][C:19]([CH2:20][NH:21][CH2:22][CH:23]([O:26][CH3:27])[O:24][CH3:25])=[CH:18][CH:17]=1.[NH2:30][C:31]1[S:32][C:33]([C:37]([NH:39][CH2:40][C:41]2[CH:42]=[N:43][CH:44]=[CH:45][CH:46]=2)=[O:38])=[C:34]([CH3:36])[N:35]=1>>[CH3:27][O:26][CH:23]([O:24][CH3:25])[CH2:22][N:21]([CH2:20][C:19]1[CH:18]=[CH:17][C:16]([F:15])=[CH:29][CH:28]=1)[C:1](=[O:2])[NH:30][C:31]1[S:32][C:33]([C:37]([NH:39][CH2:40][C:41]2[CH:42]=[N:43][CH:44]=[CH:45][CH:46]=2)=[O:38])=[C:34]([CH3:36])[N:35]=1

참가 물질

4

반응물 3

HCID 11615438N-(2,2-dimethoxyethyl)-N-(4-fluorobenzyl)amineHCID 627938962-amino-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamideHCID 63686639N-(2,2-dimethoxyethyl)-4-fluoroaniline

생성물 1

HCID 866452842-(3-(2,2-dimethoxyethyl)-3-(4-fluorobenzyl)ureido)-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide수율 69%

실험 절차

Following the procedure as described in step B of Preparation 2, making variations as required to replace N-(2,2-dimethoxyethyl)-4-fluoroaniline with N-(4-fluorobenzyl)-2,2-dimethoxyethanamine to react with 2-amino-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide, 2-(3-(2,2-dimethoxyethyl)-3-(4-fluorobenzyl)ureido)-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide was obtained in 69% yield: MS (ES+) m/z 488.4 (M+1).

후처리

  1. customas described in step B of Preparation 2

출처 및 근거

ORD 기록
ord-36338a1fb5574f3c848e5d13a9e44d79
출처 데이터셋
uspto-grants-2011_11
특허 번호
US08063084B2

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