38680-83-0Relevant academic research and scientific papers
Preparation method of 6alpha, 9alpha-difluoroprednisolone
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, (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.
Improved synthesis of fluocinolone acetonide and process research of 6α,9α-fluorination
Tang, Jie,Zeng, Chunling,Xie, Longyong,Wang, Jinghua,Tian, Mi,Guo, Cancheng
supporting information, p. 110 - 112 (2018/01/26)
An efficient and improved synthetic route of fluocinolone acetonide with combination of bio-fermentation was developed from 21-acetyloxy-17α-hydroxy-4,9(11)-diene-3,20-dione (1a). Process of the 6α and 9α fluorination steps was studied, and it was observe
A process for the preparation of intermediates fluocinone acetate
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Paragraph 0017; 0035, (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.
Acyclic amine epoxide process
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, (2008/06/13)
Acyclic amines are used to transform 9α-substituted-11β-hydroxy 21-acyloxy steroids to the corresponding 9β,11β-epoxy 21-acyloxy steroids without removal of the C17 or C21 ester. The acyclic amines are cheaper and easier to prepare than previously disclosed dehydrohalogenating agents which do not produce cleavage of the C21 ester.
