4-oxo-3-[(phenylmethyl)oxy]-4H-pyran-2-carboxylic acid
AssigneesViiV Healthcare Company, Shionogi & Co., Ltd.
InventorsBrian Alvin Johns, Jason Gordon Weatherhead, Toshikazu Hakogi, Yasunori Aoyama
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Abstract
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 RuCl3 and NaIO4 to form the compound of formula P-5.
Claims1
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
- b) treating a 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 a compound of formula P-4 with RuCl3 and NaIO4 to form a compound of formula P-5.
Dependencies are inferred from the claim text.