| abstract |
The invention discloses a preparation method of fluprogesterone acetate, which uses compound I, namely 9α-OH-AD, as a starting material, undergoes elimination reaction, cyano substitution reaction, ketal protection reaction, esterification reaction, Grignard reaction, bromine Compound VIII (16α-acetate-9-fluoro-11β-hydroxypregn-4-ene-3,20-dione) was obtained by epoxy reaction and fluorine reaction, that is, fluorine progesterone acetate. The starting material of the present invention is cheap, easy to obtain and stable, and the whole process flow is simple, and the side chain is put on the low-temperature format, which avoids the high-temperature esterification under the presence of 9 (11) epoxy, greatly reduces side reactions, and greatly The total yield is improved, the production cost is reduced, and it is more suitable for industrialized production. |