CAS: 164656-23-9; 1H-Indeno[5,4-F]Quinoline-7-Carboxamide, N-[2,5-Bis(Trifluoromethyl)Phenyl]-2,4A,4B,5,6,6A,7,8,9,9A,9B,10,11,11A-Tetradecahydro-4A,6A-Dimethyl-2-Oxo-, (4Ar,4Bs,6As,7S,9As,9Bs,11Ar)-

上下游产品

2-iodo-1,4-bis-(trifluoromethyl)-benzene 3-Oxo-4-aza-5alpha-androst-1-ene-17beta-carboxamide 20H29NO5SC20H29NO5S 2,5-bis(trifluoromethyl)aniline

黄体酮置于盐酸,Potassium Permanganate,Sodium Periodate,三甲基氯硅烷,四甲基乙二胺,Palladium 10% On Activated Carbon,三氟化硼乙醚,Potassium Tert-Butylate,氨,氢气,溴,Potassium Carbonate,对甲苯磺酸,1,8-二氮杂双环[5.4.0]十一碳-7-烯,三乙胺,Sodium Hydroxide体系中,用 四氢呋喃,1,4-二氧六环,甲醇,二氯甲烷,水,N,N-二甲基甲酰胺,乙腈,叔丁醇 用作溶剂,-20.0~78.0 °C,830.01 Kpa 条件下,反应 20.16H,反应生成度他雄胺
参考文献: Process For The Synthesis Of (5A,17ß)-N-[(2,5-Bis(Trifluoromethyl)-Phenyl]-3-Oxo-4-Aza-5-Androst-1-Ene-17-Carboxamide[fr] Procédé De Synthèse Du (5,17)-N-[(2,5-Bis(Trifluorométhyl)-Phényl]-3-Oxo-4-Aza-5-Androst-1-ène-17-Carboxamide
标题: Process For The Synthesis Of (5A,17ß)-N-[(2,5-Bis(Trifluoromethyl)-Phenyl]-3-Oxo-4-Aza-5-Androst-1-Ene-17-Carboxamide[fr] Procédé De Synthèse Du (5,17)-N-[(2,5-Bis(Trifluorométhyl)-Phényl]-3-Oxo-4-Aza-5-Androst-1-ène-17-Carboxamide
摘要:合成包括以下反应步骤:在三氢甲苯醇中存在高锰酸钾和碱金属碳酸盐的情况下,氧化孕甾-4-烯-3,20-二酮环"a"的α,β-不饱和酮系统,用亚碘酸钠,将得到的3,5-内酰胺与氯甲酸酯在0oc以下的温度下在三级有机碱的存在下反应,将得到的新化合物在隔离或不隔离的情况下与氨或乙酸铵反应,将得到的羧酰胺与酸环化,催化氢化得到的烯内酯胺,用水合二氧六环中的碱性次溴酸盐氧化得到的孕烷化合物17位侧链.然后,一方面得到的(5α,17β)-3-氧代-4-氮代-5-雄烷-17-羧酸与氯甲酸酯反应,得到的新化合物与2,5-双(三氟甲基)-苯胺在lewis酸的存在下反应,得到的酰胺在惰性气氛中与三甲基氯硅烷在ν,ν,ν',ν'-四甲基-乙二胺的存在下反应,然后向反应混合物中加入过量碘,并从乙腈中结晶得到碘化反应的产物,然后得到的2-碘代-3-氧代-4-氮代-17β-羧酰胺与叔丁基钾反应以得到最终产物.另一方面,(5α,17β)-3-氧代-4-氮代-5-雄烷-17-羧酸通过已知方法转化为甲酯,这后者通过已知方法转化为甲基(2α,5α,17β)-2-碘代-3-氧代-4-氮代-5-雄烷-17-羧酸酯,得到的化合物与叔丁基钾反应,得到的(5α,17β)-3-氧代-4-氮代-5-雄-1-烯-17-羧酸与氯甲酸酯反应,然后得到的新化合物在lewis酸催化剂的存在下与2,5-双(三氟甲基)-苯胺偶联以获得最终产物.

专利信息

专利号:US-2015239796-A1
优先权日:2014-02-19
标题:One pot synthesis of 18f labeledtrifluoromethylated compounds with difluoro(iodo)methane
发明人：RüHL THOMAS; RISS PATRICK; RAFIQUE WAQAS
权利人:UNIV OSLO
摘要:The present invention relates to compositions and methods for the synthesis of 18 F labeled compounds. In particular, the present invention relates to a copper (I) mediated one pot method for 18 F-trifluoromethylation of aromatic- or heteroaromatic halides with difluoro(iodo)methane (e.g., for use at PET imaging agents).

专利号:WO-2013001322-A1
优先权日:2011-06-30
标 题:PROCESS FOR THE SYNTHESIS OF (5α,17β)-N-[(2,5-BIS(TRIFLUOROMETHYL)-PHENYL]-3-OXO-4-AZA-5-ANDROST-1-ENE-17-CARBOXAMIDE
发明人：SOEROES BELA; TUBA ZOLTAN; GALIK GYOERGY; MAHO SANDOR; BALOGH LASZLO; VINCZE PETER; HORVATH JANOS; KOVACS ANDRAS; BENI ZOLTAN; VARGA FRIGYES
权利人:RICHTER GEDEON NYRT; SOEROES BELA; TUBA ZOLTAN; GALIK GYOERGY; MAHO SANDOR; BALOGH LASZLO; VINCZE PETER; HORVATH JANOS; KOVACS ANDRAS; BENI ZOLTAN; VARGA FRIGYES
摘要:The synthesis consists of reaction steps as follows: oxidizing the α,β-unsaturated ketone system of ring 'A' of pregn-4-ene-3,20-dion- of formula (II) with sodium metaperiodate in tert-butanol in the presence of potassium permanganate and alkali metal carbonate, reacting the obtained 3,5-seco acid with an ester of chloroformic acid in the presence of tertier organic base below 0°C, reacting the obtained new compound after isolation or without isolation with ammonia or ammonium acetate, cyclization of the resulting carboxamides with an acid, cathalytic hydrogenating the obtained ene lactame, and oxidizing the side chain at position 17 of the obtained pregnane compound with an alkali metal hypobromide in aqueous dioxane below 10°C. Thereafter on one hand the obtained (5α,17β)-3-oxo-4-aza-5-androstane-17-carboxylic acid is reacted with chloroformic acid ester, the obtained new compound is reacted with 2,5-bis(trifluoromethyl)-aniline in the presence of a Lewis acid, the obtained amide is reacted with trimethyl chlorosilane in inert atmosphere in the presence of Î ,Î ,Î ',Î '-tetramethyl-ethylendiamine, then en excess iodine is added to the reaction mixture and the product of the iodination reaction is crystallized from acetonitrile, then the obtained 2-iodo-3-oxo-4-aza-17β-carboxamide is reacted with potassium tert-butylate to furnish final product. On the other hand, (5α,17β)-3-oxo-4-aza-5-androstane-17-carboxylic acid is transformed into methylester by known method, this latter is transformed into methyl (2α,5α,17β)-2-iodo-3-oxo-4-aza-5-androstane-17-carboxylate according to known method, the obtained compound is reacted with potassium-tert-butylate, the obtained (5α,17β)-3-oxo-4-aza-5-androst-1-ene-17-carboxylic acid is reacted with an ester of chloroformic acid, then the obtained new compound is coupled with 2,5-bis(trifluoromethyl)-aniline in the presence of a Lewis acidcatalyst to gain final product.

专利号:US-12295961-B2
优先权日:2009-12-31
标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols
发明人：DHINGRA OM
权利人:MARIUS PHARMACEUTICALS INC
摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

专利号:US-2025268920-A1
优先权日:2022-04-20
标 题:Use of androgen receptor-mediated mechanisms in the treatment of acute myeloid leukemia
发明人：QIAN FENGHUA; PRABHU KUMBLE SANDEEP; PAULSON ROBERT F
权利人:PENN STATE RES FOUND
摘要:Provided is a method for treating a blood cancer in an individual in need thereof by administrating to the individual an agent that inhibits activity or expression of one or more enzymes that participate in synthesis of either or both dihydrotestosterone (DHT) or androgen receptor (AR), or an antagonist AR, or a combination of an agent and the antagonist. The methods are shown in connection with acute myeloid leukemia (AML).

专利号:US-2012295932-A1
优先权日:2011-05-17
标 题 :Method for the treatment of cancer
发明人：FERLINI CRISTIANO; MARIANI MARISA; SHAHABI SHOHREH
权利人:FERLINI CRISTIANO; MARIANI MARISA; SHAHABI SHOHREH; WESTERN CONNECTICUT HEALTH NETWORK INC
摘要:Provided is a method for determining the prognosis of cancer in a female patient with a solid tumor. Also provided is a method of sensitizing a cancer cell from a solid tumor from a male patient other than a prostate cancer cell to treatment with a chemotherapeutic agent comprising administering an effective amount ofn (a)n (i) at least one antiandrogen; (ii) at least one inhibitor of androgen synthesis; or (iii) a combination of at least one antiandrogen and at least one inhibitor of androgen synthesis; and n (b) at least one chemotherapeutic agent other than an antiandrogen or an inhibitor of androgen synthesis for the treatment of cancer characterized by a solid tumor, other than prostate cancer, in a male patient. The antiandrogen, the inhibitor of androgen synthesis, or the combination of both may be administered before, after, or at the same time as the chemotherapeutic agent.

专利号:US-12194020-B2
优先权日:2017-12-22
标 题:Reversing baldness through cannabinoid receptor activation
发明人：POSTREL RICHARD
权利人:POSTREL RICHARD
摘要:This invention reverses male pattern baldness by shocking dormant hair follicles out of their androgen induced hibernation phase back to the active hair-growing anagenic phase. The invention integrates two functions: 1) It blocks synthesis of compounds holding the follicles in the telogenic/hibernating phase and 2) It stimulates synthesis of compounds animating the hair-growing/anagenic phase in the follicular activity cycle. One preferred embodiment comprises an enzyme inhibitor blocking the conversion of testosterone to dihydrotestosterone (DHT), a flavonoid simultaneously increasing synthesis of prostaglandins alternative to prostaglandin D2, and a selected cannabinoid compound stimulating restore the hair follicle to its normal growth cycle. This novel trimodal therapy restores the hair follicles to their normal cycling processes and maintains these restorative properties so long as this rebalance in maintained.