CAS: 90357-06-5; N-(4-Cyano-3-(Trifluoromethyl)Phenyl)-3-((4-Fluorophenyl)Sulfonyl)-2-Hydroxy-2-Methylpropanamide

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CAS号90356-78-8 N-[4-氰基-3-(三氟甲基... | CAS号371-42-6 4-氟苯硫酚 | CAS号90357-51-0 2-羟基-2-甲基-N-[4-... | CAS号455-15-2 4-氟苯基甲基砜 | CAS号87310-69-8 N-[4-氰基-3-(三氟甲基... | CAS号824-80-6 对氟苯亚磺酸钠 | CAS号937-14-4 间氯过氧苯甲酸 | CAS号216665-25-7 N-[4-cyano-3-(t... | CAS号1067225-62-0 4-cyano-3-(trif... | CAS号432-98-4 1-(4-fluorophen...

N-[4-氰基-3-(三氟甲基)苯基]甲基环氧丙烯酰胺置于sodium Hydride,间氯过氧苯甲酸体系中,用 二氯甲烷 作为反应溶剂,化学反应 32.25H,反应生成 比卡鲁胺
参考文献:非甾体类抗雄激素.2-羟基丙酰苯胺的3-取代衍生物的合成及构效关系.
标题:非甾体类抗雄激素.2-羟基丙酰苯胺的3-取代衍生物的合成及构效关系.
摘要:制备了一系列3-(取代的硫代)-2-羟基丙酰苯胺和一些相应的通式(7)的砜和亚砜,其中r'是甲基或三氟甲基,并测试了其抗雄激素活性.三氟甲基系列(7,R'= Cf3)的成员通常表现出部分雄激素激动剂活性,而甲基系列(7,R'= Ch3)的成员是纯拮抗剂.甲基系列中的铅优化导致发现了新型的,有效的抗雄激素药,它们在外围具有选择性.(rsi-4'-氰基-3-[(4-氟苯基)磺酰基]-2-羟基-2-甲基-3'-(三氟甲基)丙酰苯胺40(ici 176334)目前正在开发中用于治疗雄激素反应性良性和恶性疾病.
DOI:10.1021/jm00400A011

专利信息

专利号:US-11873305-B2
优先权日:2020-06-30
标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds
发明人：ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES
权利人:GENENTECH INC; HOFFMANN LA ROCHE
摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-7199257-B1
优先权日:1999-06-10
标题 :Process for the synthesis of N-(4-cyano-3-trifluoromethylphenyl)-3-(4-fluorophenylsulfonyl)-2-hydroxy-2-methylpropionamide
发明人：SOEROES BELA; TUBA ZOLTAN; GALIK GYOERGY; BOR ADAM; DEMETER ADAM; TRISCHLER FERENC; HORVATH JANOS; BRLIK JANOS
权利人:RICHTER GEDEON VEGYESZET
摘要:A new process is disclosed for the synthesis of racemic or optically pure N-[4-cyano-3-trifluoro-methyl-phenyl]-3[4-fluorophenyl-sulfonyl]-2-hydroxy-2-methylpropionamide. The process includes the formation of several novel intermediates in the synthesis.

专利号:US-7759520-B2
优先权日:1996-11-27
标 题 :Synthesis of selective androgen receptor modulators
发明人：DALTON JAMES T; MILLER DUANE D; YIN DONGHUA; HE YALI
权利人:UNIV TENNESSEE RES FOUNDATION
摘要:The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:US-6995284-B2
优先权日:2000-08-24
标题 :Synthesis of selective androgen receptor modulators
发明人：DALTON JAMES T; MILLER DUANE D; HE YALI; YIN DONGHUA
权利人:UNIV TENNESSEE RES FOUNDATION
摘要:The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.