Solid forms comprising 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione and a coformer, compositions and methods of use thereof
US-2017258778-A1 · Sep 14, 2017 · US
US8940912B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-8940912-B2 |
| Application number | US-201314044258-A |
| Country | US |
| Kind code | B2 |
| Filing date | Oct 2, 2013 |
| Priority date | Jul 25, 2008 |
| Publication date | Jan 27, 2015 |
| Grant date | Jan 27, 2015 |
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The present invention features a process for the preparation of 4-oxo-3-[(phenylmethyl)oxy]-4-H-pyran-2-carboxylic acid, an intermediate useful in the synthesis of HIV integrase inhibitors. The process involves (a) treating a compound of formula P-2 with lithium bis(trimethylsilyl)amide and benzaldehyde to form a compound of formula P-3, (b) treating the compound of formula P-3 with triethylamine and methanesulfonyl chloride followed by N-methyl-2-pyrrolidone and 1,8-diazabicyclo[5.4.0]undec-7-ene to form a compound of formula P-4, and (c) treating the compound of formula P-4 with RuCl 3 and NaIO 4 to form the compound of formula P-5.
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The invention claimed is: 1. A process for the preparation of a compound of formula P-5 comprising the steps of: a) treating a compound of formula P-2 with lithium bis(trimethylsilyl)amide and benzaldehyde to form a compound of formula P-3…
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