3-噻吩甲酰氯置于三乙胺体系中,用 甲苯 作为反应溶剂,25.0~750.0 °C,133.32 Pa 条件下,反应 3.0H,反应生成 3-乙炔基噻吩 参考文献:Aitken,R. Alan; Horsburg,Caroline E. R.; Mccreadie,J. Graeme,Journal Of The Chemical Society. Perkin Transactions I,1994,# 13,P. 1727-1732 标题:Aitken,R. Alan; Horsburg,Caroline E. R.; Mccreadie,J. Graeme,Journal Of The Chemical Society. Perkin Transactions I,1994,# 13,P. 1727-1732
专利号:US-8487109-B2 优先权日:2007-07-03 标题:Process for the palladium-catalyzed coupling of terminal alkynes with aryl tosylates 发明人:RKYEK OMAR; NAZARE MARC; LINDENSCHMIDT ANDREAS; URMANN MATTHIAS; HALLAND NIS; ALONSO JORGE 权利人:RKYEK OMAR; NAZARE MARC; LINDENSCHMIDT ANDREAS; URMANN MATTHIAS; HALLAND NIS; ALONSO JORGE; SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), n nwherein R1; R2; R3; R4; R5; J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process for aryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional aryl-1-alkynes of the formula I.
专利号:US-8420812-B2 优先权日:2007-07-03 标题:Process for the palladium-catalyzed coupling of terminal alkynes with heteroaryl tosylates and heteroaryl benzenesulfonates 发明人:RKYEK OMAR; NAZARE MARC; LINDENSCHMIDT ANDREAS; ALONSO JORGE; URMANN MATTHIAS; HALLAND NIS 权利人:RKYEK OMAR; NAZARE MARC; LINDENSCHMIDT ANDREAS; ALONSO JORGE; URMANN MATTHIAS; HALLAND NIS; SANOFI SA 摘要:A process for the palladium-catalyzed coupling of terminal alkynes with heteroaryl tosylates and heteroaryl benzenesulfonates n The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), n nwherein D, J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process of heteroaryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional heteroaryl-1-alkynes of the formula I.
专利号:US-2022048879-A1 优先权日:2020-08-13 标 题:Synthesis of small molecules inspired by Phomoxanthone A 发明人:ALI RAMEEZ; MATTSON ANITA 权利人:WORCESTER POLYTECH INST 摘要:Methods, compositions, and kits are provided for synthesizing bioactive chromane, the method including: constructing a tertiary ether stereocenter enantioselectively by catalyzed alkynylation of a substituted chromenone to obtain a chromanone; reducing alkyne and ketone in the chromanone to obtain a chroman; and converting ester to methyl group thereby obtaining chromane.
专利号:EP-1551403-B1 优先权日:2002-10-10 标 题 :5-substituted 2h-pyrazone-3-carboxylic acid derivatives as antilipolytic agents for the treatment of metabolic-related disorders such as dyslipidemia 发明人:SEMPLE GRAEME; AVERBUJ CLAUDIA; SKINNER PHILIP; GHARBAOUI TAWFIK; SHIN YOUNG-JUN 权利人:ARENA PHARM INC 摘要:The present invention relates to certain pyrazole carboxylic acid derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, as antilipolytic agents and against for the receptor RUP25, wherein: R2 is H, halogen, C1-12 alkyl or C1-12 haloalkyl; and R3 is C3-6 cycloalkyl, C1-12 alkyl, C1-12 haloalkyl, C3-6 cycloalkyl-C1-4-alkylene, aryl-C1-4-alkylene or heteroaryl-C1-4-alkylene, wherein said aryl-C1-4-alkylene and heteroaryl-C1-4-alkylene can be optionally substituted 1 to 5 substituents selected from the substituents listed in the claims. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for pharmaceutical compositions in combination with other active agents, for example, those agents belonging to the class of alpha-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, thiazolidinedione and the like.
专利号:US-9803240-B2 优先权日:2008-04-01 标题 :Stabilized nucleic acid dark quencher-fluorophore probes 发明人:COOK RONALD M; LYTTLE MATT 权利人:BIOSEARCH TECH INC 摘要:The present invention provides a new class of solids supports for synthesis of modified oligomers of nucleic acids, and nucleic acid probes that have a format expediently synthesized on the new supports. Exemplary solid supports include at least one quencher bound through a linker to the solid support. Various exemplary embodiments include a moiety that stabilizes a duplex, triplex or higher order aggregation (e.g., hybridization) of nucleic acids of which the oligomer of the invention is a component. Other components of the solid support include moieties that stabilize aggregations of nucleic acids, e.g., intercalators, minor groove binding moieties, bases modified with a stabilizing moiety (e.g., alkynyl moieties, and fluoroalkyl moieties), and conformational stabilizing moieties, such as those described in commonly owned U.S. Patent Application Publication No. 2007/0059752.
专利号:CN-113582797-B 优先权日:2021-08-17 标 题:A method of copper-catalyzed synthesis of trifluoromethyl-1,3-enyne compounds
参考标题:Diversity Oriented Clicking (Doc): Divergent Synthesis Of Sufexable Pharmacophores From 2‐substituted‐alkynyl‐1‐sulfonyl Fluoride (Sasf) Hubs 作者:Christopher J. Smedley,Gencheng Li,Andrew S. Barrow,Timothy L. Gialelis,Marie‐claire Giel,Alessandra Ottonello,Yunfei Cheng,Seiya Kitamura,Dennis W. Wolan,K. Barry Sharpless,John E. Moses |发布日期:2020.7.20 摘要:Diversity Oriented Clicking (Doc) Is A Unified Click‐approach For The Modular Synthesis Of Lead‐like Structures Through Application Of The Wide Family Of Click Transformations. Doc Evolved From The Concept Of Achieving "Diversity With Ease" , By Combining Classic C−c π‐bond Click Chemistry With Recent Developments In Connective Sufex‐technologies. We Showcase 2‐substituted‐alkynyl‐1‐sulfonyl Fluorides
合成参考文献
摘要:Yoshida, H., Science of Synthesis Knowledge Updates, (2022) 3, 16. 摘要:Clark, R. W.; Wiskur, S. L., Science of Synthesis Knowledge Updates, (2015) 1, 43. 摘要:Delvos, L. B.; Oestreich, M., Science of Synthesis Knowledge Updates, (2017) 1, 86. 摘要:Krause, N.; Arisetti, N., Science of Synthesis Knowledge Updates, (2020) 3, 104. 摘要:Wu, X.-F., Science of Synthesis Knowledge Updates, (2014) 1, 302.