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Piconol → N-((R)-2-cyclopropyl-2-hydroxy-propyl)-5-(4-fluoro-phenyl)-6-(pyridin-2-ylmethoxy)-nicotinamide

HRID 1766567
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HRID 1766567 반응식
Br[C:2]1[CH:3]=[C:4]([C:9]([OH:11])=O)[CH:5]=[N:6][C:7]=1Cl.[N:12]1[CH:17]=[CH:16][CH:15]=[CH:14][C:13]=1[CH2:18][OH:19].[F:20][C:21]1[CH:26]=[CH:25][C:24](B(O)O)=[CH:23][CH:22]=1.[NH2:30][CH2:31][C@@:32]([CH3:37])([CH:34]1[CH2:36][CH2:35]1)[OH:33]>>[CH:34]1([C@:32]([OH:33])([CH3:37])[CH2:31][NH:30][C:9](=[O:11])[C:4]2[CH:3]=[C:2]([C:24]3[CH:25]=[CH:26][C:21]([F:20])=[CH:22][CH:23]=3)[C:7]([O:19][CH2:18][C:13]3[CH:14]=[CH:15][CH:16]=[CH:17][N:12]=3)=[N:6][CH:5]=2)[CH2:36][CH2:35]1
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참가 물질

5

반응물 4

HCID 11474PiconolHCID 2854335-Bromo-6-chloropyridine-3-carboxylic acidHCID 2856454-Fluorophenylboronic acidHCID 51684102(2R)-1-amino-2-cyclopropyl-propan-2-ol

생성물 1

HCID 24856917N-((R)-2-cyclopropyl-2-hydroxy-propyl)-5-(4-fluoro-phenyl)-6-(pyridin-2-ylmethoxy)-nicotinamide

실험 절차

The title compound was synthesized in analogy to Example 75, using 5-bromo-6-chloro-3-pyridinecarboxylic acid, 2-pyridinemethanol, (4-fluoro-phenyl)-boronic acid and (R)-α-(aminomethyl)-α-methyl-cyclopropanemethanol as starting materials to yield N-((R)-2-cyclopropyl-2-hydroxy-propyl)-5-(4-fluoro-phenyl)-6-(pyridin-2-ylmethoxy)-nicotinamide, MS (ISP) 422.0 (M+H)+.

후처리

  1. customThe title compound was synthesized in analogy to Example 75

출처 및 근거

ORD 기록
ord-894bfd0a792f4f9ea706d603928fa2b3
출처 데이터셋
uspto-grants-2007_06
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US07229999B2

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