CAS: 24916-90-3; Dexamethasone 9,11-Epoxide

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CAS号78761-59-8 11alpha,17,21-t... | CAS号89561-92-2 16α-methyl-3,20... | CAS号2884-51-7 21-o-acetyl dex... | CAS号83919-23-7 糠酸莫米松 | CAS号105102-22-5 莫美他松

21-O-乙酰基地塞米松9,11-环氧化物置于水,Sodium Hydroxide体系中,用 甲醇,二氯甲烷 用作溶剂,化学反应 3.0H,反应生成地塞米松环氧水解物
参考文献:皮质类固醇21-乙酰氧基-17α-羟基-16α-甲基-Pregna-1,4,9(11)-三烯-3,20-二酮合成的改进及其在一些与地塞米松和地塞米松有关的杂质合成中的常用中间体莫米松.
标题:皮质类固醇21-乙酰氧基-17α-羟基-16α-甲基-Pregna-1,4,9(11)-三烯-3,20-二酮合成的改进及其在一些与地塞米松和地塞米松有关的杂质合成中的常用中间体莫米松.
摘要:与地塞米松或莫米松有关的杂质相当多,这些杂质不能由相应的活性药物成分制成,而只能由常见的中间体21-乙酰氧基-17α-羟基-16α-甲基-孕烯-1,4,9(11)-三烯-3,20-二酮(12).这样,该关键中间体的稳健而经济的合成对于为这些杂质提供有弹性且经济可行的供应链至关重要.因此,至关重要的是要有一个健壮且经济可行的方法来以非常好的收率和质量合成中间体12.我们在这里报告了从这种常见中间体中合成的12种和8种与地塞米松和莫米松有关的杂质的改进方法.
Doi:10.1016/j.Steroids.2019.04.008

专利信息

专利号:EP-1422235-B1
优先权日:2001-07-26
标题 :Stereoselective method of producing 6alpha-fluoropregnanes and intermediaries
发明人：MURILLO GARRIDO JOSE VICENTE; SILVA GUISASOLA LUIS OCTAVIO; MARTIN JUAREZ JORGE
权利人:RAGACTIVES SL
摘要:6 alpha -fluorpregnanes (I), where the dotted line between positions 1 and 2 represents a single or double bond; R1 is OH, OCOR2, X, SO3R3, or an (R7)(R8)(R9)SiO- group, where X is halogen, R2 and R3 are C1-6 alkyl or phenyl optionally substituted by C1-4 alkyl, and R7, R8 and R9, equal or different, are C1-6 alkyl or phenyl optionally substituted by C1-4 alkyl, can be obtained by means of a high stereoselectivity process comprising reacting a 3-(trisubstituted)silyloxy-pregna-3,5-diene (IV) with a fluorinating agent selected among N-fluorosulfonimides and N-fluorosulfonamides. The 6 alpha -fluorpregnanes (I) are intermediates for the synthesis of steroids useful as anti-inflammatory and anti-asthmatic agents.

专利号:US-4188322-A
优先权日:1978-04-28
标题 :Process for the preparation of 6-halo-pregnanes
发明人：CASTELLI PIER P; ROMANO BRUNO
权利人:BLASINACHIM SPA
摘要:The invention relates to a new process for the preparation of 6α-halo-3-keto-Δ 1 ,4 -pregnadiene-derivatives in two-steps-synthesis affording directly 6α-halo-derivatives by reacting 3-keto-9β,11β-oxido-Δ 1 ,4 -pregnadiene-derivatives with a suitable acylating or etherifying agent to give the corresponding new 3-enol-derivatives which are finally halogenated by using a suitable halogenating agent.