Antifungal compound process
The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
1. A compound of formula XI:
each R 4 is independently H or halo;
o is 1, 2, or 3
each R 5 is independently H or fluoro;
each R 6 is independently H or fluoro;
each R 11 is independently halo or
and
each R 12 is independently H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl, or optionally substituted hetrocyclyl.
2. The compound of claim 1 , wherein the compound has the following formula:
wherein each R 1 is independently, halo or
3. A process to prepare compound 2-5,
comprising:
(i) reacting ester 6,
with morpholine to provide morpholine amide 7:
(ii) reacting morpholine amide 7:
to provide ketone 3,
(iii) performing olefination of ketone 3,
to provide olefin 2-5,
wherein M is Mg or MgX; and X is halogen; and
each R 1 is independently, halo or