Antifungal Compound Process
AssigneesMycovia Pharmaceuticals, Inc., The United States of America, as represented by the Secretary, Department of Health and Human Serv
InventorsWilliam J. Hoekstra, Christopher M. Yates, Mark Behnke, Asaf Alimardanov, Scott A. David, Douglas Franklin Fry
Life of this patent
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Abstract
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.
Claims7
1-21. (canceled)
A process to prepare enantio-enriched amino-alcohol 1-6* or 1-7*,
- or a mixture thereof, the method comprising:
- (i) reacting ester 2,
- with morpholine to provide morpholine amide 2b,
- (ii) displacing the morpholino portion of morpholine amide 2b,
- to provide ketone 3,
- (iii) forming the epoxide of ketone 3,
- to provide epoxide 4,
- (iv) ring-opening epoxide 4,
- to provide amino-alcohol ±4b,
- (v) enriching the enantiomeric purity of amino-alcohol ±4b,
- to provide enantio-enriched amino-alcohol 4b or 4c:
- or a mixture thereof;
- and
- (vi) arylating enantio-enriched amino-alcohol 4b or 4c,
- or a mixture thereof, to provide enantio-enriched aryl-pyridine 1-6* or 1-7*,
- or a mixture thereof;
- wherein each R1 is independently halo or
(canceled)
A process to prepare enantio-enriched amino-alcohol 4b or 4c:
- or a mixture thereof, the method comprising:
- (i) reacting ester 2,
- with morpholine to provide morpholine amide 2b,
- (ii) displacing the morpholino portion of morpholine amide 2b,
- to provide ketone 3,
- (iii) forming the epoxide of ketone 3,
- to provide epoxide 4,
- (iv) ring-opening epoxide 4,
- to provide amino-alcohol ±4b,
- and
- (v) enriching the enantiomeric purity of amino-alcohol ±4b,
- to provide enantio-enriched amino-alcohol 4b or 4c:
- or a mixture thereof;
- wherein each R1 is independently halo or
(canceled)
A process to prepare enantio-enriched amino-alcohol 4b or 4c:
- or a mixture thereof, the method comprising:
- (i) enriching the enantiomeric purity of amino-alcohol ±4b,
- to provide enantio-enriched amino-alcohol 4b or 4c:
- or a mixture thereof;
- wherein each R1 is independently halo or
27-58. (canceled)
Dependencies are inferred from the claim text.