碘代环戊烷置于碘苯,四丁基溴化铵体系中,用 四氯化碳,乙腈 用作溶剂,化学反应生成溴代环戊烷 参考文献:Breslow,Ronald; Canary,James W.,Journal Of The American Chemical Society,1991,Vol. 113,# 10,P. 3950-3951 标题:Breslow,Ronald; Canary,James W.,Journal Of The American Chemical Society,1991,Vol. 113,# 10,P. 3950-3951
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-2025132776-A1 优先权日:2023-12-20 标题 :Use of iron-based compounds for the synthesis of borated compounds, and corresponding methods 发明人:HANNEDOUCHE JÉRÔME; BEZZENINE SOPHIE; GIL RICHARD; CHEN DONGHUANG; WOWK VINCENT 权利人:UNIV PARIS SACLAY; CENTRE NAT RECH SCIENT 摘要:The present invention relates to the use of iron-based compounds for the synthesis of borated compounds, and the corresponding methods.
专利号:US-6147226-A 优先权日:1999-02-16 标题 :Synthesis of cyclopentyl 2-thienyl ketone, tiletamine and tiletamine acid addition salts, such as tiletamine hydrochloride 发明人:LAPIN YURI ALEKSANDROVICH; SANCHEZ IGNACIO H 权利人:GREAT LAKES CHEMICAL CORP 摘要:A water-scavenging solvent, such a polyphosphoric acid, can be used for the synthesis of cyclopentyl 2-thienyl ketone by the direct acylation of cyclopentanecarboxylic acid without first reacting the cyclopentanecarboxylic acid with thionylchloride to form the acid chloride, while achieving new and unexpected yields. A tiletamine-free base can be made from the cyclopentyl 2-thienyl ketone with a halide in the presence of a solvent for the cyclopentyl 2-thienyl ketone to form a halogenated cyclopentane 2-thienyl ketone, aminating the halogenated cyclopentane 2-thienyl ketone by reaction with an amine, and subjecting the reaction product to thermal rearrangement, in a suitable solvent, and at a sufficient temperature to form tiletamine free base. Each step for the formation of tiletamine free base can be accomplished using the same solvent, e.g., dichlorobenzene so that intermediates need not be isolated between reactions.
专利号:US-5969159-A 优先权日:1999-02-16 标 题 :Synthesis of cyclopentyl 2-thienyl ketone tiletamine and tiletamine acid addition salts such as tiletamine hydrochloride 发明人:LAPIN YURI ALEKSANDROVICH; SANCHEZ IGNACIO H 权利人:GREAT LAKES CHEMICAL CORP 摘要:Solid, non-tin-containing catalysts can be used for the synthesis of cyclopentyl 2-thienyl ketone by the reaction of cyclopentanecarboxylic acid chloride and thiophene, while achieving new and unexpected yields. Aluminum trichloride is both cheaper than stannic chloride and it is easier to deal with as a waste stream. The successful use of graphite as a catalyst for the reaction of cyclopentanecarboxylic acid chloride and thiophene provides a mild and ecologically friendly method for carrying out the Friedel-Crafts reaction. A tiletamine-free base can be made from the cyclopentyl 2-thienyl ketone with a halide in the presence of a solvent for the cyclopentyl 2-thienyl ketone to form a halogenated cyclopentane 2-thienyl ketone; aminating the halogenated cyclopentane 2-thienyl ketone by reaction with an amine; and subjecting the reaction product to thermal rearrangement, in a suitable solvent, and at a sufficient temperature to form tiletamine free base. Each step for the formation of tiletamine free base can be accomplished using the same solvent, e.g., dichlorobenzene so that intermediates need not be isolated between reactions.
专利号:US-3708547-A 优先权日:1969-09-02 标 题 :Synthesis of(10)-annulenes 发明人:NELSON P; UNTCH K 权利人:SYNTEX CORP 摘要:NEW PROCESS FOR PREPARING (10)-ANNULENE COMPOUNDS WHICH ARE USEFUL AS ESTROGENIC, ANTI-INFLAMMATORY, AND ANTI-FERTILITY AGENTS. THE PROCESS UTILIZES THE STEPS OF ADDING A METHANO, DICHLOROMETHANO, OR DIFLUOROMETHAO GROUP ACROSS THE C-9,10 DOUBLE BOND OF A 1,4,5,8-TETRAHYDRONAPHTHALENE TO THE CORRESPONDIG 9,10-BRIDGED-1,45,8,9,10-HEXAHYDRONAPHTHLENE AND TREATING THE LATTER WITH A BENZOQUINONE TO THE CORRESPONDING 1,6-BRIDGED(10)-ANNULENE PRODUCT. THE PREPARATINS OF 1,6-METHANO(10)-ANNULENE, 1,6-DICHLOROMETHANO-(10)-ANNULENE, AND 1,6-DIFLUOROMETHANE-(10)-ANNULENE ARE ILLUSTRATED AS REPRESENSTATIVE OF THE PROCESS.
专利号:US-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
摘要:Kantchev, E. A. B.; Organ, M. G., Science of Synthesis, (2009) 48, 32. 摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 172. 摘要:Braun, M., Science of Synthesis Knowledge Updates, (2017) 1, 447. 摘要:Guram, A. S.; Milne, J. E.; Tedrow, J. S.; Walker, S. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 119. 摘要:Park, K.; Jo, H., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 909.