Methanol → Methyl 3-(benzyloxy)-4-oxo-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidine-2-carboxylate

HRID 2426256

反応式

HRID 2426256 の反応式
Cl.[NH:2]=[C:3]1[CH2:8][CH2:7][CH2:6][CH2:5][NH:4]1.[O:9]=[C:10](CC([O-])=O)[C:11]([O-:13])=O.[CH2:18]1[CH2:28][CH2:27]N2[C:21](=NCCC2)[CH2:20][CH2:19]1.C[CH2:30][O:31][C:32]([CH3:34])=[O:33].[CH3:35]O>>[CH2:35]([O:13][C:11]1[C:10](=[O:9])[N:4]2[CH2:5][CH2:6][CH2:7][CH2:8][C:3]2=[N:2][C:34]=1[C:32]([O:31][CH3:30])=[O:33])[C:21]1[CH:20]=[CH:19][CH:18]=[CH:28][CH:27]=1

参加物

6

反応物 5

HCID 887MethanolHCID 8857Ethyl AcetateHCID 811841,8-Diazabicyclo(5.4.0)undec-7-eneHCID 164550OxalacetateHCID 178479080HCID 178479080、化合物

生成物 1

HCID 59771042Methyl 3-(benzyloxy)-4-oxo-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidine-2-carboxylate

実験手順

Commercially available 2-iminopiperidine hydrochloride (1.5 eq) was added at room temperature to a solution of oxosuccinate prepared in Step 1 b (1 eq) in MeOH. After dropwise addition of neat DBU (4.5 eq), the reaction mixture was stirred for 2 days. Evaporation of the solvent gave a residue that was taken into EtOAc and washed with 1N HCl and brine; the organic layer was dried on Na2SO4 and the solvent removed. The crude was used without further purification.

後処理

  1. customEvaporation of the solvent
  2. customgave a residue that
  3. washwashed with 1N HCl and brine
  4. customthe organic layer was dried on Na2SO4
  5. customthe solvent removed
  6. customThe crude was used without further purification

出典と根拠

ORDレコード
ord-cadc7bedb6f049e8ac365a03c6d488fa
出典データセット
uspto-grants-2011_06
特許番号
US07968553B2

関連ノート

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