CAS: 393-11-3; 4-Nitro-3-(Trifluoromethyl)Aniline

上下游产品

CAS号384-22-5 2-硝基-Alpha,Alph... | CAS号13311-84-7 氟他胺 | CAS号393-09-9 5-氟-2-硝基三氟甲苯 | CAS号351-36-0 3-乙酰氨基三氟甲苯 | CAS号393-12-4 4'-硝基-3'-(三氟甲基)乙酰苯胺 | CAS号1058742-35-0 2,4-二氟-4-羟基-N-(... | CAS号325-14-4 7-三氟甲基喹啉 | CAS号344-62-7 2'-(三氟甲基)乙酰苯胺 | CAS号364-13-6 2-(三氟甲基)-1,4-亚苯基二胺 | CAS号52806-53-8 羟基氟他胺 | CAS号384-22-5 2-硝基-Alpha,Alph... | CAS号444-29-1 2-碘三氟甲苯 | CAS号445-03-4 2-氨基-5-氯三氟甲苯 | CAS号445-04-5 4-氨基-3-三氟甲基苯酚 | CAS号444-30-4 邻三氟甲基苯酚

氟他胺置于盐酸体系中,用 甲醇,水 作为反应溶剂,化学反应 0.4H,反应生成 5-氨基-2-硝基三氟甲苯
参考文献:Ph和温度对氟他胺稳定性的影响.用ei +-Ms 进行HPLC研究并鉴定降解产物
标题:Ph和温度对氟他胺稳定性的影响.用ei +-Ms 进行HPLC研究并鉴定降解产物
摘要:使用新的经过验证的稳定性指示HPLC方法研究了氟他胺(flt)的化学稳定性.使用甲醇-磷酸盐缓冲液(0.04 M,Ph 4.0)(75:25,V / V)的流动相,在240 Nm处进行uv检测,在c 18色谱柱上将flt与降解产物分离.该方法在0.2-25.0μgml-1的浓度范围内对flt表现出优异的线性.发现flt在缓冲的酸性和碱性溶液中易于降解.将flt在水溶液中的降解动力学评估为ph和温度的函数.在酸性和碱性条件下,分别在70-100和60-90oc的温度范围内,Flt的降解遵循一级动力学和arrhenius行为.在2.0-12.0的ph范围内研究了ph速率曲线,在ph 3.0-5.0时具有最大的稳定性.计算出flt水解的活化能为79.4和52.0 Kj Mol-1Ph分别为0.5(0.3 M Hcl)和12.5(0.03 M Naoh).通过质谱法鉴定出4-硝基-3-三氟甲基
DOI:10.1039/c4Ra13617A

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