CAS: 65-04-3; 17α-Methyl-1-Testosterone

上下游产品

2α-bromo-17β-hydroxy-17α-methyl-5α-androstan-3-one (223)C05451ZIN(223)C05451 Epiandrosterone mestanolone oxandrolone

美雄诺龙置于甲烷磺酸,2-Iodoxybenzoic Acid体系中,用 N,N-二甲基乙酰胺,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 13.0H,反应生成 17Alpha-甲基异睾酮
参考文献:一种氧雄龙中间体的制备方法
标题:一种氧雄龙中间体的制备方法
摘要:本发明属于有机合成技术领域.本发明提供了一种17β‑羟基‑17α‑甲基‑1‑氧代‑1,2‑开环‑a失碳‑5α‑雄甾‑2‑含氧羧酸的制备方法,包括如下步骤:1)将美雄诺龙,2‑碘酰基苯甲酸,催化剂和溶剂混合后进行氧化反应,得到化合物1;2)将化合物1,氧化剂水溶液,碳酸氢盐和丙酮混合后进行氧化反应,得到17β‑羟基‑17α‑甲基‑1‑氧代‑1,2‑开环‑a失碳‑5α‑雄甾‑2‑含氧羧酸.本发明的制备方法所得到产品的纯度>=98%,收率为95~97%;本发明的制备方法所需的反应温度低,同时显著缩短了反应时间,产品生产周期短,操作简单,生产成本降低,绿色环保.

专利信息

专利号:US-6448413-B1
优先权日:1999-06-10
标题:Process for the synthesis of a-nor-seco compounds with sterane skeleton
发明人：SANTA CSABA; TUBA ZOLTAN; MAHO SANDOR; SZELES JANOS; BALOGH GABOR; BRLIK JANOS; TRISCHLER FERENC; SZILAGYI GABRIELLA; BAKCSI ERIKA
权利人:RICHTER GEDEON VEGYESZET
摘要:The invention relates to a new process for the synthesis of 17β-hydroxy-17α-methyl-1,3-seco-2-nor-5α-androstane-3-acid derivatives of formula (I) n wherein the meaning of Z is carboxyl or formyl group and n to the new secoindoxylidene carboxylic acid derivatives of formula (II) n wherein R 1 and R 2 independently are C 1 -C 4 alkyl or alkoxy group, hydrogen or halogen atom—which are intermediates for preparing the compounds of formula (I). n The 17β-hydroxy-17α-methyl-1,3-seco-2-nor-5α-androstane-3-acid derivatives of formula (I) are intermediates in the synthesis of oxandrolon (17β-hydroxy-17α-methyl-2-oxa-5α-androstane-3-one), which is used as anabolic in therapy.

专利号:US-6583298-B1
优先权日:1999-06-10
标 题:Process for the synthesis of 17β-hydroxy-17α-methyl-2-oxa-5α-androstane-3-one
发明人：SANTA CSABA; TUBA ZOLTAN; MAHO SANDOR; SZELES JANOS; FERENCZI KATALIN; HORVATH PETER; LANCOS KRISZTINA; MESTER TAMAS; TROMPLER ARPAD
权利人:RICHTER GEDEON VEGYESZET
摘要:The invention relates to a new process for the synthesis of 17β-hydroxy-17α-methyl-2-oxa-5α-androstane-3-one of formula (I). The process according to the invention is as follows: the 17β-hydroxy-17α-ethyl-1,3-seco-2-nor-5α-androstane-1,3-diacid of formula (III) is transformed into the ring-closed 17β-hydroxy-17α-methyl-1,3-seco-2-nor-5α-androstane-1,3-diacid anhydride of formula (II) in an inert solvent or without solvent with a C 2 -C 3 alkan acid anhydride or a substituted carbodiimide of formula R 1 —Nâ•?Câ•?N—R 2 — wherein R 1 and R 2 independently are C 1 -C 6 alkyl group, C 1 -C 6 alkyl group substituted by tertiary or quaternary amino group or 1-3 phenyl group, C 5 -C 6 cycloalkyl group, aryl group substituted by 1-3 methoxy, tertiary amino, nitro, C 1 -C 4 alkyl group or 1-3 halogen atom—and the obtained compound of formula (II) is reduced regioselectively by a complex alkali metal hydride in an inert solvent The new 17β-hydroxy-17α-methyl-1,3-seco-2-nor-5α-androstane-1,3-diacid anhydride of ormula (II) is also the subject of the invention.

专利号:US-2003032817-A1
优先权日:2001-05-15
标题:Process for the synthesis of oxandrolone
发明人：CABAJ JOHN E; KAIRYS DAVID L; ZIZELMAN PAUL M
摘要:A process is disclosed for synthesizing oxandrolone 1 involving the bromination of compound 2 to obtain compound 3, followed by the highly selective de-bromination of compound 3 to obtain compound 4, followed by the oxidation of compound 4 to obtain compound 6, and finally the reduction of compound 6 to obtain oxandrolone 1.

专利号:US-7009063-B2
优先权日:2001-12-11
标题:Process for the production of oxandrolone
发明人：DESAI SHAILESHKUMAR RAMANLAL; RAY JR DAVID WAYNE; SAYED YOUSRY A
权利人:BARR LAB INC
摘要:The present invention relates to a process for the synthesis of oxandrolone from mestanolone. The process comprises the steps of: (a) oxidizing mestanolone to form 17β-hydroxy-17α-methyl-5α-androst-1-en-3-one; (b) hydroxylating the 17β-hydroxy-17α-methyl-5α-androst-1-en-3-one to form 1α, 2α, 17β-trihydroxy-17α-methylandrostan-3-one; (c) cleaving the 1α, 2α, 17β-trihydroxy-17α-methylandrostan-3-one to form 17β-hydroxy-17α-methyl-1-oxo-1,2,-seco-A-nor-5α-androstan-2-oic acid; and (d) reducing the 17β-hydroxy-17α-methyl-1-oxo-1,2,-seco-A-nor-5α-androstan-2-oic acid to form oxandrolone.

专利号:EP-1189885-B1
优先权日:1999-06-10
标题:Process for the synthesis of a-nor-seco compounds with sterane skeleton

专利号:WO-02100881-A1
优先权日:2001-05-15
标 题:Process for the synthesis of oxandrolone