Method for the preparation of 6alpha-fluoro corticosteroids
A method for producing a 6 -fluorinated corticosteroid or derivative thereof by reacting a 17-hydroxy-21-ester epoxide of Formula II 1 with a stereoselective fluorinating agent to stereoselectively form a 21-ester-17-hydroxy 6 -fluorinated compound of Formula VII 2 R 1 can be OC(O)-R d ; R 4 can be...
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Format: | Patent |
Sprache: | eng |
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Zusammenfassung: | A method for producing a 6 -fluorinated corticosteroid or derivative thereof by reacting a 17-hydroxy-21-ester epoxide of Formula II
1
with a stereoselective fluorinating agent to stereoselectively form a 21-ester-17-hydroxy 6 -fluorinated compound of Formula VII
2
R
1
can be OC(O)-R
d
; R
4
can be C(O)-R
d
; R
3
can be H or R
d
. Each R
d
may be the same or different and is independently selected from (C
1-4
)alkyl, aryl and heteroaryl. The dashed line can be a single or a double bond. R
4
may be, for example, acetyl; R
3
may be, for example, alpha or beta methyl; R
4
may be, for example, acetate or propionate. The stereoselective fluorinating agent used in the reaction may be, for example, a fluoropyridinium or fluoroquinuclidium compound, for example, Selectfluor®. |
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