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HRID 924115作成日:2026年10月26日

2,6-Difluoropyridine-4-boronic acid → (R)-2',6'-Difluoro-2-(3-hydroxypyrrolidin-1-yl)-N-(4-(trifluoromethoxy)phenyl)-[3,4'-bipyridine]-5-carboxamide

https://huagongshe.com/reaction/924115

反応式

関与物質

役割名称HCID仕込み量
反応物2,6-Difluoropyridine-4-boronic acidHCID 2762747—
反応物(R)-5-bromo-6-(3-hydroxypyrrolidin-1-yl)-N-(4-(trifluoromethoxy)phenyl)nicotinamideHCID 86702593—
生成物(R)-2',6'-Difluoro-2-(3-hydroxypyrrolidin-1-yl)-N-(4-(trifluoromethoxy)phenyl)-[3,4'-bipyridine]-5-carboxamideHCID 118195169—

反応手順

The title compound was prepared in an analogous fashion to that described in Example 169 using (R)-5-bromo-6-(3-hydroxypyrrolidin-1-yl)-N-(4-(trifluoromethoxy)phenyl)nicotinamide (Stage 35.1) and 2,6-difluoropyridin-4-ylboronic acid to afford a white amorphous powder. HPLC (Condition 4) tR=5.67 min, UPLC-MS (Condition 3) tR=1.10 min, m/z=481.1 [M+H]+; 1H-NMR (400 MHz, DMSO-d6) δ ppm 1.70-1.80 (m, 1H) 1.87 (m, J=9.00 Hz, 1H) 2.86 (d, J=11.34 Hz, 1H) 3.18-3.29 (m, 2H) 3.47 (m, J=7.00 Hz, 1H) 4.22 (br. s, 1H) 4.87 (d, J=3.52 Hz, 1H) 7.23 (s, 2H) 7.34 (d, J=9.38 Hz, 2H) 7.78-7.89 (m, 2H) 8.13 (d, J=2.35 Hz, 1H) 8.78 (d, J=2.35 Hz, 1H) 10.18 (s, 1H).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09278981B2
出典データセットuspto-grants-2016_03
ORD IDord-fa83b769f2164fb485d08ffa2cf1a8db
出典メモuspto-grants-2016_03