氟替卡松丙酸酯 [CAS80474-14-2]合成路线图解——原料药厂家东康源(3)

更多原料药产品信息请百度东康源原料药。

Reference 2:

phillips, g.h.; bain, b.m.; williamson, c.; steeples, i.p.; laing, s.b. (glaxo wellcome plc);

androstane 17beta-carbothioates. gb 2088877; nl 8100707; us 4335121 .

Reference 3:

castaner, j.; prous, j.; fluticasone propionate. drugs fut 1991, 16, 5, 424.

Route 2

new methods for the synthesis of fluticasone propionate have been reported:1) the reaction of

6alpha,9alpha-difluoro-11beta,17alpha-dihydroxy-16alpha-methyl-3-oxo and

rosta-1,4-diene-17beta-carboxylic acid (i) with carbonyldiimidazole (cdi) and h2s in dmf gives

the corresponding carbothioic acid (ii), which is selectively acylated with propionyl chloride

and triethylamine in ch2cl2, yielding the 17alpha-propionyloxy derivative (iii). the reaction of

(iii) with ch2brcl and nahco3 in dma affords the s-chloromethyl ester (iv), which by reaction with

nai in refluxing acetone is converted to the s-iodomethyl ester (v). finally, this compound is

treated with agf in acetonitrile.2) by esterification of thioacid (ii) with bromofluoromethane

or fluoroiodomethane by means of k2co3 in dmf.

搜索“diyifanwen.net”或“第一范文网”即可找到本站免费阅读全部范文。收藏本站方便下次阅读，第一范文网，提供最新外语学习氟替卡松丙酸酯 [CAS80474-14-2]合成路线图解——原料药厂家东康源(3)全文阅读和word下载服务。