N,N-Diisopropylmethylamine → (R)-methyl 2-(4-chloro-2-(2,4-dimethoxybenzyl)-7-fluoro-3-oxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-6-ylamino)-4-methylpentanoate

HRID 516105

反応式

HRID 516105 の反応式
[Cl:1][C:2]1[C:7]2[C:8](=[O:22])[N:9]([CH2:11][C:12]3[CH:17]=[CH:16][C:15]([O:18][CH3:19])=[CH:14][C:13]=3[O:20][CH3:21])[CH2:10][C:6]=2[C:5]([F:23])=[C:4](Cl)[N:3]=1.Cl.[NH2:26][C@@H:27]([CH2:32][CH:33]([CH3:35])[CH3:34])[C:28]([O:30][CH3:31])=[O:29].C(N(C)C(C)C)(C)C>C(#N)C>[Cl:1][C:2]1[C:7]2[C:8](=[O:22])[N:9]([CH2:11][C:12]3[CH:17]=[CH:16][C:15]([O:18][CH3:19])=[CH:14][C:13]=3[O:20][CH3:21])[CH2:10][C:6]=2[C:5]([F:23])=[C:4]([NH:26][C@H:27]([CH2:32][CH:33]([CH3:35])[CH3:34])[C:28]([O:30][CH3:31])=[O:29])[N:3]=1

参加物

5

反応物 3

HCID 547370N,N-DiisopropylmethylamineHCID 2723695Leucine methyl ester hydrochlorideHCID 583175754,6-dichloro-2-[(2,4-dimethoxyphenyl)methyl]-7-fluoro-1H,2H,3H-pyrrolo[3,4-c]pyridin-3-one

生成物 1

HCID 58317585(R)-methyl 2-(4-chloro-2-(2,4-dimethoxybenzyl)-7-fluoro-3-oxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-6-ylamino)-4-methylpentanoate

試薬・触媒・溶媒 1

HCID 6342Acetonitrile溶媒

反応条件

温度
100 °C

実験手順

A mixture of 4,6-dichloro-2-(2,4-dimethoxybenzyl)-7-fluoro-1H-pyrrolo[3,4-c]pyridin-3(2H)-one (3 g, 8.08 mmol), (S)-methyl 2-amino-4-methylpentanoate hydrochloride (2.94 g, 16.16 mmol), and N-isopropyl-N-methylpropan-2-amine (3.76 mL, 24.25 mmol) in ACN (50 mL) was stirred at 100° C. for 3 d. The solvent was removed and the resulting residue was used in the next step without further purification. [M+H] calc'd for C23H27ClFN3O5, 480; found, 480.

後処理

  1. customThe solvent was removed
  2. customthe resulting residue was used in the next step without further purification

出典と根拠

ORDレコード
ord-f841ab9bc87148b4adf520ab514a5b35
出典データセット
uspto-grants-2015_08
特許番号
US09108970B2

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