Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Phosphate | HCID 1061 | — |
| Reactant | (R)-5-(3-chlorophenyl)-3-(1-((4-Methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)oxy)ethyl)isoxazole | HCID 16041426 | — |
| Solvent | Ethanol | HCID 702 | — |
| Product | 934338-70-2 | HCID 69004954 | — |
Reaction Steps
The salt manufactured at 1 g scale from ethanol was further investigated for its intrinsic dissolution rate and compared to the free base of 4-(5-{(1R)-1-[5-(3-chlorophenyl)isoxazol-3-yl]ethoxy}-4-methyl-4H-1,2,4-triazol-3-yl)pyridine. The salt had a 1000 times higher intrinsic dissolution rate as compared to the free base. Dissolution rates of the base and salt were measured with a low-volume rotating disc method. Discs were compressed from pure compound and centrically mounted in a disc holder with an exposed area of 0.07 cm2. The disc holder rotated at 500 rpm immersed in 50 mL USP Phosphate buffer pH 6.8 at 37° C. The compound was analyzed UV-Online by a Spectrophotometer with a flow cell and a peristaltic pump with continuous circulation.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US07476684B2 |
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| Source dataset | uspto-grants-2009_01 |
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| ORD ID | ord-d6caf126ba9b4ae4a3b7551802effbfe |
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| Source note | uspto-grants-2009_01 |
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