2-硝基苯基硼酸置于palladium On Activated Charcoal 氢气体系中,用 四氢呋喃,乙醇 用作溶剂,化学反应生成2-氨基苯硼酸频哪醇酯 参考文献:Self-Activation And 1,8-Stereoinduction In A Boronate-Substituted Dienophile 标题:Self-Activation And 1,8-Stereoinduction In A Boronate-Substituted Dienophile 摘要:发现邻硼代苯胺亲双烯体 4 与环戊二烯的 [4+2] 环加成反应比其对位异构体 8 和未取代的衍生物 6 进行得更快,从而证实了在 4 的情况下,通过内部配位的自激活是有效的. 手性硼酸酯衍生物9和10提供了小水平的远程1,8-立体诱导.这些结果表明,二烷氧基硼酸酯可以作为弱的内路易斯酸,并在环加成反应中活化含羰基的官能团. Doi:10.1055/s-2002-20470
专利号:US-12384788-B2 优先权日:2019-09-13 标 题 :1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine derivatives and related compounds as LRRK2, NUAK1 and/or TYK2 kinase modulators for the treatment of e.g. autoimmune disease 发明人:KOESTLER ROLAND; TASSEL JEAN; THORMANN MICHAEL; YEHIA NASSER; TREML ANDREAS; ALMSTETTER MICHAEL 权利人:ORIGENIS GMBH 摘要:The present invention relates to compounds of formula (I) that are capable of modulating, e.g., inhibiting or activating, one or more kinases, especially LRRK2 and/or NUAK1 and/or TYK2 or mutants thereof. The compounds are useful for treating diseases, such as autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, Alzheimer's disease, Parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 40 to 146; examples 1 to 63; compounds 1 to 248; tables 1 to 3). Preferred compounds are e.g. 1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine derivatives and related compounds. An exemplary compound is e.g. 5-(2,6-difluorophenyl)-8-methoxy-1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine (example 49). (Formula (II):
专利号:US-8389732-B2 优先权日:2006-03-29 标题 :Synthesis and regioselective substitution of 6-halo- and 6-alkoxy nicotine derivatives 发明人:COMINS DANIEL L; WAGNER FLORENCE F; ONDACHI PAULINE 权利人:COMINS DANIEL L; WAGNER FLORENCE F; ONDACHI PAULINE; UNIV NORTH CAROLINA STATE 摘要:The present invention provides active compounds for modulating nicotinic acetylcholine receptors and methods of making the same. The methods of preparing the active compounds utilize different intermediate compounds.
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-2007232665-A1 优先权日:2006-03-29 标题 :Synthesis and regioselective substitution of 6-halo-and 6-alkoxy nicotine derivatives
专利号:US-7989438-B2 优先权日:2007-07-17 标题 :Therapeutic compounds 发明人:CONTE IMMACOLATA; HABERMANN JOERG; MACKAY ANGELA; NARJES FRANK; RICO FERREIRA MARIA DEL ROSARIO; STANSFIELD IAN 权利人:ANGELETTI P IST RICHERCHE BIO 摘要:A class of macrocyclic compounds of formula (I), wherein R 7 , A, Ar, B, D, F, M, Q 1 , Q 2 , W, X, Y and Z are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.
专利号:US-2013131015-A1 优先权日:2006-03-29 标 题 :Synthesis and regioselective substitution of 6-halo- and 6-alkoxy nicotine derivatives
参考标题:Palladium-Catalyzed Regioselective Synthesis Of 3-Arylindoles From N -Ts-Anilines And Styrenes 作者:So Won Youn,Tae Yun Ko,Young Ho Jang |发布日期:2017.6.1 摘要:A Pd-Catalyzed Intermolecular Oxidative Annulation Between N-Ts-Anilines And Styrenes Was Developed. This Method Offers A Straightforward And Robust Approach To A Wide Range Of 3-Arylindoles Using Readily Available Starting Materials With Good Functional-Group Tolerance And High Regioselectivity And Efficiency. Further Elaboration Of The Products Obtained From This Process Provided Access To Highly
合成参考文献
摘要:Suginome, M.; Ohmura, T., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 149. 摘要:Murata, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 449. 摘要:Zhang, F.-L.; Wang, Y.-F., Science of Synthesis, (2021) , 398.