Summary
The invention describes a novel process amenable for the large-scale practical synthesis of cis-tetrahydro-furo[2,3-b]furan-3-one. This compound is useful as a key intermediate for the synthesis of highly potent and resistance-repellent HIV protease inhibitors that share a common component called bis-tetrahydrofuran (bis-THF). Specifically, the invention provides a method of preparing these precursors by modification of reaction temperatures, conditions and reagents leading to increased yields and purity of the desired intermediates. Such modifications would be useful in the large-scale preparation of highly potent and resistance-repellent HIV protease inhibitors currently under development as antiviral agents useful in treating AIDS.
Feb. 1, 2012
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