CAS: 401900-40-1; (2S)-3-(4-Acetamidophenoxy)-2-Hydroxy-2-Methyl-N-[4-Nitro-3-(Trifluoromethyl)Phenyl]Propanamide

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4-acetaminophenol (S)-N-(4-nitro-3-(trifluoromethyl)phenyl)-2-methyloxirane-2-carboxamide N-[4-nitro-3-(trifluoromethyl)phenyl]-(2R)-3-bromo-2-hydroxy-2-methylpropanamide 4-nitro-3-(trifluoromethyl)benzeneamine

5-氨基-2-硝基三氟甲苯置于氯化亚砜,Caesium Carbonate体系中,用 四氢呋喃 作为反应溶剂,化学反应 29.58H,反应生成 N-[4-硝基-3-(三氟甲基)苯基]-(2S)-3-[4-(乙酰基氨基)苯氧基]-2-羟基-2-甲基丙酰胺
参考文献:Methods Of Treating Urological Disorders Using Sarms
标题:Methods Of Treating Urological Disorders Using Sarms
摘要:本发明涉及通过给予本发明的sarm化合物来治疗,预防,抑制和/或抑制尿路疾病,如尿失禁,包括压力性尿失禁和盆底障碍的方法.

专利信息

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-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.

专利号:US-7968721-B2
优先权日:2003-01-13
标 题:Large-scale synthesis of selective androgen receptor modulators
发明人：MILLER DUANE D; VEVERKA KAREN A; CHUNG KIWON
权利人:UNIV TENNESSEE RES FOUNDATION
摘要:This invention relates to a process for preparing a selective androgen receptor modulator (SARM) compound represented by the structure of formula I: n nwherein X is O; and T, Z, Y, Q, R and R 1 are defined herein. The process includes coupling between an amide of formula II and a phenol of formula IIIn n n n n n n n n n n nfollowed by a purification step consisting of precipitating the compound of formula (I) in a mixture of alcohol and water alone.

专利号:US-2004014975-A1
优先权日:2000-08-24
标 题:Synthesis of selective androgen receptor modulators

专利号:US-2006009529-A1
优先权日:1996-11-27
标 题:Synthesis of selective androgen receptor modulators

专利号:ES-2420129-T3
优先权日:2003-01-13
标题 :Large-scale synthesis of selective androgen receptor modulators