- Preparation method for fluocortolone
-
The invention relates to a preparation method for fluocortolone; through a Grignard reaction of a compound represented by the formula I, fluocortolone represented by the formula II is generated. The preparation method for fluocortolone is simple in route and easy to operate, has the raw material easy to obtain, and greatly reduces production costs and industrialized conditions.
- -
-
Paragraph 0029; 0030
(2018/03/25)
-
- 9α-dehalogenation process
-
The present invention involves improved processes for the dehalogenation of 9α-halosteroids (I) STR1 to produce the corresponding 11β-hydroxy steroids (II) STR2 which are known to be useful as pharmaceutical, where the improvements comprise (1) adding the 9α-halo steroid (I) to the chromium and (2) using catalytic amounts of chromium in the presence of a means of converting chromium (II) to chromium (III).
- -
-
-
- Trimethyl siloxane steroid intermediates
-
A procedure for converting steroids characterized by presence of an 11βOH group into potent corticoids having one or more substituents, such as 6αF, 16α, 17α-hydroxy or isopropylidene dioxy, 16α or 16β methyl, Δ1,4 ; by reacting the 11β-hydroxy steroid with trichloromethyl siloxane steroid, thereby rendering the normally sensitive 11 substituent inert to the series of reactions which thereafter incorporate one or more of the desired above listed substituents into the steroid molecule. The siloxy group is then hydrolyzed to regenerate the 11β-hydroxy substituent. Many of the trimethyl siloxy steroids are novel compounds. The siloxane may be selectively cleaved by reaction of the finely divided steroid with 40-60% aqueous HF.
- -
-
-