CAS: 521-18-6; 17β-Hydroxy-5α-Androstan-3-One

上下游产品

testosterone androstanedione 17β-hydroxy-5α-androstan-3-one semicarbazone 5alpha-Androstane-3beta,17beta-diol-17-hexahydrobenzoatedihydrotestosterone p-chlorophenoxyisobutyrate 2-(4-Chloro-phenoxy)-2-methyl-propionic acid (5S,10R,13S,17S)-3-[2-(4-chloro-phenoxy)-2-methyl-propionyloxy]-10,13-dimethyl-2,5,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl ester dihydrotestosterone propionate Propionic acid (5S,10R,13S,17S)-10,13-dimethyl-17-propionyloxy-2,5,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl ester

睾酮置于吉拉尔特试剂 T,三氟乙酸体系中,用 甲醇 作为反应溶剂,化学反应 1.0H,反应生成 雄诺龙
参考文献:质谱成像对小鼠睾丸中雄激素的空间定位和定量.
标题:质谱成像对小鼠睾丸中雄激素的空间定位和定量.
摘要:雄激素对男性发育和生殖功能至关重要.它们作为血液传播的内分泌激素被运送到它们的作用部位,但也可以在组织内产生,以内分泌和旁分泌方式起作用.因此,循环浓度可能无法准确反映特定组织微环境中的雄激素影响.质谱成像允许直接从组织表面对小分子种类进行区域分析.然而,由于电离差和局部离子抑制,类固醇激素难以检测.在这里,用 Girard T 试剂衍生化用于对睾酮和 5α-二氢睾酮进行电荷标记,从而可以在小鼠睾丸,基础和最大刺激状态以及大鼠前列腺中直接检测这些类固醇.检测限为~0.1 Pg 用于睾酮.内源性类固醇的示例性检测是通过基质辅助激光解吸电离和傅里叶变换离子回旋共振检测(空间分辨率为 150 μm)或四极飞行时间检测(空间分辨率为 50 μm)实现的.通过液体萃取表面分析和电喷雾电离后的碰撞诱导碎裂来实现结构确认.该应用拓宽了组织表面衍生化策略的范围,以阐明健康和疾病中的局部内分泌信号.内源性类
DOI:10.1021/acs.Analchem.6B02242

专利信息

专利号:US-10751419-B2
优先权日:2014-05-01
标题:Method for synthesis of reactive conjugate clusters
发明人：MIGAWA MICHAEL T; YU JINGHUA; WAN W BRAD; PATEL SAYTEN P; VASQUEZ GUILLERMO; KINBERGER GARTH A; PRAKASH THAZHA P; SETH PUNIT P; SWAYZE ERIC E
权利人:IONIS PHARMACEUTICALS INC
摘要:Provided herein are improved methods for the synthesis of reactive conjugate clusters and intermediates used in such methods. In particular, improvements are provided that enhance the synthesis of reactive conjugate clusters by reducing the number of synthetic steps required. The reactive conjugate clusters prepared using the improved methods don't include any transacylation impurities that are formed using existing methods. The improved methods also provide an increase in overall yield and a cost benefit over existing methods.

专利号:US-10065985-B2
优先权日:2015-02-03
标题 :Method for fully automated synthesis of 16β-18F-fluoro-5α-dihydrotestosterone (18F-FDHT)
发明人：MURPHY JENNIFER MARIE; LAZARI MARK SAUL
权利人:UNIV CALIFORNIA
摘要:The automated synthesis of clinically relevant amounts of 16β- 18 F-fluoro-5α-dihydrotestosterone ( 18 F-FDHT) using a commercially available radiosynthesizer. Synthesis was performed in 90 minutes with a decay-corrected radiochemical yield of 29±5%. The specific activity was 4.6 Ci/μmol (170 GBq/μmol) at end of formulation with a starting activity of 1.0 Ci (37 GBq). The formulated 18 F-FDHT yielded sufficient activity for multiple patient doses and passed all quality control tests required for routine clinical use.

专利号:WO-9517903-A1
优先权日:1993-12-28
标 题:Modular design and synthesis of oxazolone-derived molecules
发明人：HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG
权利人:ARQULE PARTNERS L P; HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG
摘要:The design and synthesis of novel oxazolone-derived molecular modules and the use of the modules in the construction of new molecules and fabricated materials is disclosed. The new molecules and fabricated materials are molecular recognition agents useful in the design and synthesis of drugs, and have applications in separations and materials science.

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-12146136-B2
优先权日:2020-03-26
标题:Synthesis of modified oligonucleotides with increased stability
发明人：KHVOROVA ANASTASIA; ROUX LOÃ?C MAURICE RENÉ JEAN; YAMADA KEN
权利人:UNIV MASSACHUSETTS
摘要:This disclosure relates to the synthesis of novel modified oligonucleotides. The synthesis of novel phosphoramidites are also provided.

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.