Lactic Acid → HCID 135856772, compound

HRID 645439Notes

Reaction equation

HRID 645439 reaction equation
[CH2:1]([O:3][C:4]1[CH:9]=[CH:8][C:7]([S:10]([N:13]2[CH2:18][CH2:17][N:16]([CH3:19])[CH2:15][CH2:14]2)(=[O:12])=[O:11])=[CH:6][C:5]=1[C:20]1[NH:25][C:24](=[O:26])[C:23]2=[C:27]([CH3:33])[N:28]=[C:29]([CH2:30][CH2:31][CH3:32])[N:22]2[N:21]=1)[CH3:2].[C:34]([OH:39])(=[O:38])[CH:35]([CH3:37])[OH:36]>CCOCC.O>[C:34]([OH:39])(=[O:38])[CH:35]([CH3:37])[OH:36].[CH2:1]([O:3][C:4]1[CH:9]=[CH:8][C:7]([S:10]([N:13]2[CH2:14][CH2:15][N:16]([CH3:19])[CH2:17][CH2:18]2)(=[O:12])=[O:11])=[CH:6][C:5]=1[C:20]1[NH:25][C:24](=[O:26])[C:23]2=[C:27]([CH3:33])[N:28]=[C:29]([CH2:30][CH2:31][CH3:32])[N:22]2[N:21]=1)[CH3:2]

Participants

5

Reactant 2

HCID 612Lactic AcidHCID 135544141N-Desethyl-N-Methyl Vardenafil

Product 1

HCID 135856772HCID 135856772, compound

Reagents, catalysts & solvents 2

HCID 962WaterSolventHCID 3283Diethyl EtherSolvent

Procedure

100 mg (0.211 mmol) of 2-[2-ethoxy-5-(4-methyl-piperazine-1-sulphonyl)-phenyl]-5-methyl-7-propyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one are suspended in 5 ml of ether and admixed with 20 mg of an 85% strength solution of lactic acid in water. The mixture is stirred at room temperature for 10 minutes and evaporated to dryness. The residue is titrated with ether and filtered off with suction. This gives 110 mg (92%) of 2-[2-ethoxy-5-(4-methyl-piperazine-1-sulphonyl)-phenyl]-5-methyl-7-propyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one lactate.

Workup

  1. customevaporated to dryness
  2. filtrationfiltered off with suction

Sources & evidence

ORD record
ord-27c8216dc375430cbfcaac578c5d056e
Source dataset
uspto-grants-2010_04
Patent number
US07704999B2

Reaction notes

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