专利号:WO-2023233371-A1 优先权日:2022-06-03 标 题:A continuous flow process for synthesis of organic azides 发明人:GNANAPRAKASAM BOOPATHY; PANDEY AKANKSHA M; MONDAL SHANKHAJIT 权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES PUNE IISER PUNE 摘要:The present disclosure relates generally to the field of synthetic organic chemistry. More specifically, the disclosure is directed to a continuous flow process for synthesis of azides from alcohols and peroxides, wherein the process comprises azidation with trimethylsilyl azide and a catalyst Amberlyst-15. It is a non-hazardous, mild and controlled reaction giving good yields of azides. The azides can be further employed for synthesis of medicinally and industrially useful chemicals.
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-8431712-B2 优先权日:2004-02-09 标 题 :Methods for the synthesis of pyridoxamine 发明人:KHALIFAH RAJA G; KEILITZ ROLAND; KOELLNER CHRISTOPH; DEGENHARDT THORSTEN; BRAND STEPHEN ROBERT 权利人:KHALIFAH RAJA G; KEILITZ ROLAND; KOELLNER CHRISTOPH; DEGENHARDT THORSTEN; BRAND STEPHEN ROBERT; NEPHROGENEX INC 摘要:The invention provides non-oxidative methods for the large scale manufacture of pyridoxamine (I) (4-aminomethyl-3-hydroxy-5-hydroxymethyl-2-methylpyridine): n nand salts thereof.n nThe invention also provides intermediate compounds for the synthesis of pyridoxamine, as well as compositions and methods for the treatment and/or prevention of conditions associated with the formation of post-Amadori advanced glycation end-products.
专利号:US-2004101523-A1 优先权日:1989-07-27 标题:Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension 发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J 权利人:SEARLE & CO 摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.
专利号:WO-9101724-A1 优先权日:1989-07-27 标题 :Renal-selective prodrugs for the treatment of hypertension 发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J 权利人:SEARLE & CO 摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as depa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitors compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-Y-glutamyl fusaric acid is preferred.
专利号:US-2008207908-A1 优先权日:2007-01-29 标 题:Processes for the preparation of piperidinyl-substituted urea compounds 发明人:GLESS RICHARD D 权利人:ARETE THERAPEUTICS INC 摘要:Disclosed are processes for the synthesis of piperidinyl-substituted urea compounds. This invention further relates to novel intermediates prepared during this synthesis.
摘要:Inagi, S.; Taniguchi, K.; Lam, K., Science of Synthesis: Modern Strategies in Organofluorine Chemistry, (2024) 2. 参考文献:10.1007/s00438-002-0653-x 摘要:Nomura T, Ishihara A, Imaishi H, Endo TR, Ohkawa H, Iwamura H. Molecular characterization and chromosomal localization of cytochrome P450 genes involved in the biosynthesis of cyclic hydroxamic acids in hexaploid wheat. Mol Genet Genomics. 2002 Apr;267(2):210–7. doi: 10.1007/s00438-002-0653-x.