专利号:US-5254776-A 优先权日:1992-07-17 标 题:Synthesis of bromobiphenyls 发明人:LANG JOHN F; GURUSAMY NARAYANASAMY 权利人:MALLINCKRODT SPEC CHEM 摘要:Bromobiphenyls (such as 2-fluoro-4-bromobiphenyl) are synthesized by reacting together a phenylboronic acid (such as phenylboronic acid) and a bromoiodobenzene (such as 2-fluoro-4-bromoiodobenzene). The reaction generally takes place with the aid of a catalyst (such as palladium in a zero valance state) and an inert solvent (such as fluorobenzene). Control of temperature is very important to obtain both an acceptable reaction rate and an acceptable level of terphenyl byproduct.
专利号:WO-2024185814-A1 优先权日:2023-03-06 标题:Method for producing aryl compound containing tritylsulfanyl group 发明人:OKAZOE TAKASHI; NOZAKI KYOKO; GATZENMEIER Tim; LIU YUE 权利人:AGC INC; UNIV TOKYO 摘要:The present invention provides: a substrate for achieving the highly efficient synthesis of an aryl compound containing a tritylsulfanyl group; a method for producing a compound containing an SF 5 group using the substrate; and others. The present invention is a method for producing an aryl compound containing a tritylsulfanyl group, the method comprising thiotritylating a halogenated aryl compound represented by general formula (1) [wherein A 1 represents an aryl group that may have a substituent or a heteroaryl group that may have a substituent; and X represents a halogen atom] using [(triphenylmethyl)sulfanyl]potassium or [(triphenylmethyl)sulfanyl]sodium to produce an aryl compound containing a tritylsulfanyl group, the aryl compound being represented by general formula (2) [wherein A 1 is the same as A 1 in general formula (1); and Ph represents a phenyl group].
专利号:US-7122694-B2 优先权日:1998-11-06 标 题 :Hydroboronation process 发明人:MARCUCCIO SEBASTIAN MARIO; RODOPOULOS MARY; WEIGOLD HELMUT 权利人:BORON MOLECULAR PTY LTD 摘要:The invention relates to processes for the synthesis of aryl or alkene borates which comprises reacting: (i) an olefinic compound having a halogen or halogen-like substituent in a vinylic substitution position, or (ii) an aromatic ring having a halogen or halogen-like substituent in a ring substitution position, with a disubstituted monohydroborane in the presence of a Group 8-11 metal catalyst. The invention also relates to the use of these borates in coupling reactions. The invention further relates to certain disubstituted monohydroboranes and aryl or alkene borates.
专利号:US-6017926-A 优先权日:1997-12-17 标题 :Integrin receptor antagonists 发明人:ASKEW BEN C; COLEMAN PAUL J; DUGGAN MARK E; HALCZENKO WASYL; HUTCHINSON JOHN H; MEISSNER ROBERT S; PATANE MICHAEL A; WANG JIABING 权利人:MERCK & CO INC 摘要:The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors alpha v beta 3, alpha v beta 5 and/or alpha v beta 6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, and tumor growth and metastasis.
专利号:US-9550757-B2 优先权日:2010-03-05 标题:Nuclear transport modulators and uses thereof 发明人:SHACHAM SHARON; KAUFFMAN MICHAEL; SANDANAYAKA VINCENT P; SHECHTER SHARON 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).
专利号:CN-102030651-A 优先权日:2009-09-28 标题:Synthesis method of 2-fluo-4-bromobiphenyl ethyl formate
参考标题:Synthesis Of α-Aryl Nitriles Through Palladium-Catalyzed Decarboxylative Coupling Of Cyanoacetate Salts With Aryl Halides And Triflates 作者:Rui Shang,Dong-Sheng Ji,Ling Chu,Yao Fu,Lei Liu |发布日期:2011.5.2 摘要:Worth Its Salt: The Palladium‐catalyzed Decarboxylative Coupling Of The Cyanoacetate Salt As Well As Its Mono‐ And Disubstituted Derivatives With Aryl Chlorides, Bromides, And Triflates Is Described (See Scheme). This Reaction Is Potentially Useful For The Preparation Of A Diverse Array Of α‐aryl Nitriles And Has Good Functional Group Tolerance. S‐phos=2‐(2,6‐dimethoxybiphenyl)Dicyclohexylphosphine)
合成参考文献
摘要:Amatore, M.; Aubert, C.; Malacria, M.; Petit, M., Science of Synthesis Knowledge Updates, (2012) 3, 48. 摘要:Marsden, S. P., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 586. 摘要:Elie, M.; Renaud, J.-L.; Gaillard, S., Science of Synthesis: N-Heterocyclic Carbenes in Catalytic Organic Synthesis, (2016) 1, 205. 摘要:Liao, L.; Zhang, Y.; Yu, J.-S., Science of Synthesis: Knowledge Updates, (2024) 1, 244.