CAS: 5630-53-5; Tibolone

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炔诺酮置于吡啶,N-溴代丁二酰亚胺(Nbs),硫酸,乙酸酐,溶剂黄146,乙酰氯体系中,用 水,N,N-二甲基甲酰胺,丙酮 作为反应溶剂,化学反应 19.0H,反应生成 替勃龙
参考文献:一种替勃龙的合成方法
标题:一种替勃龙的合成方法
摘要:一种替勃龙的合成方法,具体包括以下步骤:1)炔化反应:酸性脱羧物(I)甲苯溶液,通入乙炔气至原料反应得炔诺酮(II);2)酰化反应,步骤1)得到的炔诺酮(II)加入醋酐和缚酸剂,控制室温滴加乙酰氯,搅拌反应6小时至原料反应完全,得酰化物(Iii);3)上脱溴反应,酰化物反应得4,6‑二烯醋酸炔诺酮(V);4)甲基化反应,4,6‑二烯醋酸炔诺酮(V),加入醚类溶剂,降温至‑10~30°C,滴加甲基化试剂,控制温度0~5oc搅拌反应至原料反应完全得7α‑甲基醋酸炔诺酮(Vi);5)转位反应,7α‑甲基醋酸炔诺酮(Vi)反应得转位物(Vii)湿品;6)水解反应,转位物(Vii)反应得替勃龙.

专利信息

专利号:US-2005124592-A1
优先权日:2002-01-22
标 题:Tibolone in the treatment of complaints associated with the administration of drugs which prevent the synthesis of endogenous estrogen
发明人：KLOOSTERBOER HELENIUS J; BUNDRED NIGEL
摘要:Disclosed is a treatment of estrogen-deficiency related complaints in females that exhibit these complaints while they are on treatment with a drug which prevents the synthesis of endogenous estrogen. Such drugs are, e.g., anti-cancer drugs such as aromatase inhibitors. The invention resides in the use of tibolone, which has an unexpectedly beneficial working in this particular patient group in that it does not stimulate breast, while preventing bone loss and relieving climacteric complaints in a patient group in which this is more difficult than in any other group due to the nature of the concomitant cancer treatment (no circulating estrogen making for a higher severity of the complaints, the lack of effect on the estrogen receptor making for an increased risk associated with estrogenic breast stimulation once estrogen-like compounds are administered.

专利号:US-2008146656-A1
优先权日:2005-06-01
标题:Use of a steroid sulphatase inhibitor for inhibiting the synthesis of androstenedione and/or testosterone
发明人：REED MICHAEL JOHN; PUROHIT ATUL; WOO LOK WAI LAWRENCE; POTTER BARRY VICTOR LLOYD
权利人:REED MICHAEL JOHN; PUROHIT ATUL; WOO LOK WAI LAWRENCE; POTTER BARRY VICTOR LLOYD
摘要:There is provided use of a compound capable of inhibiting a steroid sulphatase enzyme (E.C.3.1.6.2) in the manufacture of a medicament for inhibiting in vivo synthesis of at least one of androstenedione and testosterone, which may be useful for the treatment of hirsutism, excess sebum production, benign breast disease, benign ovarian disease, polycystic ovarian disease and female infertility among others.

专利号:WO-2012163563-A1
优先权日:2011-05-31
标题:New strontium salts, synthesis and use thereof in the treatment of osteoporosis
发明人：MOURELLE MANCINI MARISABEL; DEL CASTILLO NIETO JUAN CARLOS
权利人:LACER SA; MOURELLE MANCINI MARISABEL; DEL CASTILLO NIETO JUAN CARLOS
摘要:The present invention relates to a strontium salt (I) wherein n is an integer which can take the values of 0 or 1 m is an integer which can take the values of 0 or 1 R is hydrogen or methyl and stereoisomers or hydrates thereof, to methods for its synthesis, and use in the treatment and/or prophylaxis of a cartilage and/or bone disease and/or conditions resulting in a dysregulation of cartilage and/or bone metabolism in a mammal.

专利号:CN-1620298-A
优先权日:2002-01-22
标 题:Tibolone in the treatment of complaints associated with the administration of drugs which prevent the synthesis of endogenous estrogen

专利号:EP-1901737-A1
优先权日:2005-06-01
标 题 :Use of a steroid sulphatase inhibitor for inhibiting the synthesis of androstenedione and/or testosterone

专利号:CA-2609818-A1
优先权日:2005-06-01
标题 :Use of a steroid sulphatase inhibitor for inhibiting the synthesis of androstenedione and/or testosterone