PREPARATION METHOD FOR DEXAMETHASONE INTERMEDIATE

WIPO Patent Application WO/2019/129309

A1

Provided is a preparation method for a dexamethasone intermediate, relating to the field of active pharmaceutical ingredient synthesis. Compound I in a buffer salt system undergoes a cyanide reaction to synthesize 17α-CN, and said product undergoes a transposition and rearrangement reaction in an inorganic weakly alkaline saline solution to synthesize 17β-CN, i.e. compound III. Compared to traditional techniques, the use of a buffer salt system for the synthesis of 17α-CN and the subsequent transposition reaction for the synthesis of 17β-CN effectively control the generation of 5-CN impurities during the reactions, thereby enhancing the reaction yield and purity and reducing production cost. The prevention invention is suitable for scaled production.

JPH0899991	MODIFIED BILE ACIDS, PROCESS FOR THEIR PREPARATION AND THEIR USE
JPS57106647	VITALLY INFLUENCING SOFT TERTIARY AMINE ESTER OF CARBOXYLIC ACID
JPH05502434	[Title of Invention] Pharmaceutical composition and its use

YANG KUN (CN)
YU CHUANYUN (CN)
ZHOU JIANLIU (CN)

PCT/CN2019/076373

July 04, 2019

February 27, 2019

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GUANGXI WONDER PHARMACEUTICAL CO LTD (CN)

C07J41/00

WO1991008218A1

1991-06-13

CN108033990A

2018-05-15

MEYER ET AL.: "Glucosides and aglucons. XIII. Methyl ester of 3(beta)-aceto- xy-16-etiocholenic acid from gitoxigenin", HELVETICA CHIMICA ACTA, 31 December 1946 (1946-12-31)
ERCOLI: "An improved method of preparing testosterone, dihydrotestosterone, and some of their esters", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 75, no. 3, 31 December 1953 (1953-12-31), pages 650 - 653, XP002415619, ISSN: 0002-7863, DOI: 10.1021/ja01099a040

CHINA TRUER IP (CN)

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