Methylamine → N-methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-amine

HRID 57523

反応式

HRID 57523 の反応式
Cl[C:2]1[CH:7]=[CH:6][C:5]([B:8]2[O:12][C:11]([CH3:14])([CH3:13])[C:10]([CH3:16])([CH3:15])[O:9]2)=[CH:4][N:3]=1.CN.C[CH2:20][N:21](C(C)C)C(C)C>O1CCOCC1>[CH3:20][NH:21][C:2]1[CH:7]=[CH:6][C:5]([B:8]2[O:12][C:11]([CH3:14])([CH3:13])[C:10]([CH3:16])([CH3:15])[O:9]2)=[CH:4][N:3]=1

参加物

5

反応物 3

HCID 6329MethylamineHCID 81531DiisopropylethylamineHCID 27947192-Chloro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine

生成物 1

HCID 56686504N-methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-amine

試薬・触媒・溶媒 1

HCID 312751,4-Dioxane溶媒

実験手順

A mixture of 2-chloro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine (200 mg, 0.84 mmol), methanamine (277 mg, 8.4 mmol), and DIPEA (0.35 mL, 2.01 mmol) in dioxane (5 mL) was stirred at room temperature for 16 hours. It was then concentrated under reduced pressure, and the residue was treated in EtOAc. The insoluble solid was removed by filtration, and the organic solution was concentrated under reduced pressure to give the title compound.

後処理

  1. concentrationIt was then concentrated under reduced pressure
  2. additionthe residue was treated in EtOAc
  3. customThe insoluble solid was removed by filtration
  4. concentrationthe organic solution was concentrated under reduced pressure

出典と根拠

ORDレコード
ord-9a28bae1fc6a40d8874fa0fae747a213
出典データセット
uspto-grants-2016_09
特許番号
US09434726B2

関連ノート

読み込み中…