38680-83-0Relevant articles and documents
Preparation method of 6alpha, 9alpha-difluoroprednisolone
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Paragraph 0022-0024; 0035; 0036, (2020/04/17)
The invention belongs to the technical field of steroid hormone preparation, and particularly relates to a preparation method of 6alpha, 9alpha-difluoroprednisolone. Anecortave dehydroacetate used asa starting raw material undergoes bromo-hydroxy epoxidation, 6-positon fluoridation, 9-position fluoridation and hydrolysis to prepare the 6alpha, 9alpha-difluoroprednisolone. The method taking the anecortave dehydroacetate as the starting raw material has the advantages of low prices, few isomers, few impurities and short reaction route.
A process for the preparation of intermediates fluocinone acetate
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, (2017/02/09)
The invention discloses a preparation method for a fluocinolone acetonide midbody, i.e., 21-acetate-9,11-epoxy-17-alpha-hydroxypregn-1,4-diene-3,20-diketone. A compound I, i.e., 11-alpha-hydroxy-ADD (androstadienedione), serves as a starting material; an elimination reaction, a cyano-substitution reaction, a siloxy protective reaction, an intramolecular nucleophilic substitution reaction, a bromo-epoxy reaction and a replacement reaction are carried out to obtain the fluocinolone acetonide midbody. The preparation method provided by the invention has the advantages that the starting material which is relatively cheap is used, the reactions in the steps are relatively easy to implement, and the yield is higher, so that the production is more economical and safe, and higher applicability for industrial production is achieved; through route design optimization, the preparation method avoids 9 (11)-double-bonded epoxidation with the existence of 21-acetate in the traditional technique, so as to avoid the 21-acetate hydrolysis, greatly improve the quality and yield of the fluocinolone acetonide midbody, and reduce the entire production cost.