专利号:US-2008103312-A1 优先权日:2006-08-29 标 题:Processes for the synthesis of 5-phenyl-1-trityl-1H-tetrazole 发明人:KANSAL VINOD K; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; LUNAGARIYA VIJAYKUMAR D 权利人:KANSAL VINOD K; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; LUNAGARIYA VIJAYKUMAR D 摘要:Provided are processes for the synthesis of 5-phenyl-1-trityl-1H-tetrazole, an intermediate useful in the synthesis of irbesartan.
专利号:US-4592874-A 优先权日:1980-05-14 标 题:Process for the synthesis of alpha-chlorinated chloroformates 发明人:CAGNON GUY C; PITEAU MARC D; SENET JEAN-PIERRE G; OLOFSON ROY A; MARTZ JONATHAN T 权利人:POUDRES & EXPLOSIFS STE NALE 摘要:Process for the synthesis of alpha -chlorinated chloroformates, and new alpha -chlorinated chloroformates. The invention relates to a new process for the manufacture of alpha -chlorinated chloroformates and, to new alpha -chlorinated chloroformates as new industrial products. The process according to the invention consists of a synthesis, by catalytic phosgenation, of alpha -chlorinated chloroformates of the formula: in which: R represents a substituted or unsubstituted hydrocarbon radical and m represents an integer superior or equal to one, this synthesis consisting in reacting phosgene with the aldehyde R-CHO)m, in the presence of a catalyst which is an organic or inorganic substance which is capable in a medium containing an aldehyde of the formula R-CHO)m, phosgene and, possibly, a solvent, of generating a pair of ions one of which is an halogenide anion and the other is a cation which is sufficiently separated from said halogenide anion so as to give to the latter a nucleophilic power enabling it to react with the function(s) aldehyde of the molecule R-CHO)m.
专利号:US-5476915-A 优先权日:1994-06-29 标题:Method for controlled synthesis of polymers 发明人:SHEA KENNETH J; WALKER JAMES R; ZHU HIUDE 权利人:UNIV CALIFORNIA 摘要:Living polymer synthesis methods for the synthesis of oligomeric and high molecular weight polymers with low polydispersity are disclosed. The disclosed methods are based on the discovery that the reaction of a ylid with an organoborane at a high ylid:borane ratio and high temperature provides for the synthesis of high molecular weight polymers with low polydispersity.
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-4824532-A 优先权日:1987-01-09 标题:Process for the electrochemical synthesis of carboxylic acids 发明人:MOINGEON MARIE-ODILE; CHAUSSARD JACQUES; TROUPEL MICHEL; SABOUREAU CHRISTOPHE 权利人:AEROSPATIALE 摘要:The invention relates to a process for the electrosynthesis of carboxylic acids of general formula R-COOH in which R is an organic radical by the electrochemical reduction, in the presence of carbon dioxide, of organic compounds corresponding to the general formula R-Y in which R is the above-mentioned organic radical and Y is a hetero atom-containing radical, the hetero atom of the radical Y, chosen from the group consisting of oxygen, nitrogen, sulphur andphosphorus, being directly linked to a carbon atom of the radical R by a single covalent linkage. When the hetero atom is nitrogen or phosphorus, the radical Y is an ammonium or phosphonium radical respectively. The anode, which is consumed during the electrosynthesis, is made of a metal chosen from the group consisting of reducing metals and their alloys, preferably made of magnesium, aluminium or zinc. This process without catalyst is very simple to perform and enables a cell with a single compartment to be employed. The carboxylic acids are commonly employed in the chemical industry, especially as intermediates for the synthesis of pharmaceutical products or of products used in plant protection.
摘要:Sellars, J. D., Science of Synthesis Knowledge Updates, (2014) 1, 400. 摘要:Margaretha, P., Science of Synthesis Knowledge Updates, (2014) 2, 426. 摘要:Scholz, U.; Dong, W.; Feng, J.; Shi, W., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 95. 摘要:Kantak, A.; DeBoef, B., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 613. 摘要:Zhang, M.; Su, W., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 104.