N-Boc-Pyrrole-2-Boronic Acid Mida Ester置于sodium Hydroxide体系中,用 四氢呋喃,水 用作溶剂,化学反应 0.33H,以89%的收率获得1-Boc-吡咯-2-硼酸 参考文献:Knapp,David M.; Gillis,Eric P.; Burke,Martin D.,Journal Of The American Chemical Society,2009,Vol. 131,P. 6961-6963 标题:Knapp,David M.; Gillis,Eric P.; Burke,Martin D.,Journal Of The American Chemical Society,2009,Vol. 131,P. 6961-6963
专利号:US-2011152313-A1 优先权日:2008-06-20 标题 :Synthesis of ageladine a and analogs thereof 发明人:KARUSO PETER HELMUTH; SHENGULE SUDHIR RAMNATHRAO 权利人:UNIV MACQUARIE 摘要:The invention describes a one pot process for synthesizing a compound of structure (I), or a tautomer thereof. A compound of structure (II), or a tautomer thereof, and an aldehyde of structure R d CHO are condensed to form a condensation product. The resulting condensation product is then oxidized in the same reaction mixture to produce the compound of structure (I) or a tautomer thereof.
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:WO-2009152584-A1 优先权日:2008-06-20 标题 :Synthesis of ageladine a and analogs thereof
专利号:US-2009137557-A1 优先权日:2005-11-22 标题 :Calcilytic Compounds 发明人:KU THOMAS WEN FU; LIN HONG; LUENGO JUAN I; MARQUIS JR ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT; YAMASHITA DENNIS S 权利人:KU THOMAS WEN FU; LIN HONG; LUENGO JUAN I; MARQUIS JR ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT; YAMASHITA DENNIS S 摘要:Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.
专利号:US-2007275968-A1 优先权日:2004-09-07 标 题 :Substituted Biphenyl Derivative 发明人:KURATA HITOSHI; NISHIMATA TOYOKI; WATANABE YUKIKO; EBISAWA MASAYUKI; FUJIMOTO TEPPEI; KOBAYASHI HIDEKI 权利人:KURATA HITOSHI; NISHIMATA TOYOKI; WATANABE YUKIKO; EBISAWA MASAYUKI; FUJIMOTO TEPPEI; KOBAYASHI HIDEKI 摘要:The present invention relates to a biaryl derivative or a pharmacologically acceptable salt thereof having an excellent collagen-synthesis inhibition activity. A biaryl derivative having a structure represented by the following General Formula (I) or a pharmacologically acceptable salt thereof: n nwherein n R 1 represents a C 6 -C 10 aryl group which is substituted with one to three group(s) each independently selected from the group consisting of a group defined by formula R-L-, a di-(C 1 -C 6 alkyl)amino group, a di-(C 1 -C 6 alkyl)aminosulfonyl group, a hydroxyaminocarbonyl group, and a halogen atom, and so on; R represents a C 1 -C 6 alkyl group, and so on; L represents a sulfonyl group, an aminosulfonyl group, or a sulfonylamino group, and so on; R 2 represents a hydrogen atom, and so on; A represents a group defined by formula (II), (III), or (IV); R 3 represents a C 1 -C 6 alkyl group, and so on; and R 4 represents a C 1 -C 6 alkyl group, and so on.
专利号:US-2007161648-A1 优先权日:2005-10-14 标 题 :Substituted dihydro-isoindolones useful in treating kinase disorders 发明人:HUGHES TERRY V; EMANUEL STUART L; RUGG CATHERINE A; CONNOLLY PETER J 权利人:HUGHES TERRY V; EMANUEL STUART L; RUGG CATHERINE A; CONNOLLY PETER J 摘要:The present invention is directed to novel substituted dihydro-isoindolone compounds of formula (I): n n nand forms thereof, wherein Ring A, X 3 , R 1 , R 2 , R 3 , R 4 and R 6 are as herein defined, and their synthesis and use as protein kinase inhibitors and interactions thereof.
摘要:Lubell, W. D.; St-Cyr, D. J.; Dufour-Gallant, J.; Hopewell, R.; Boutard, N.; Kassem, T.; Dörr, A.; Zelli, R., Science of Synthesis Knowledge Updates, (2013) 1, 307. 摘要:Kwiecień, H., Science of Synthesis Knowledge Updates, (2018) 3, 210. 摘要:Khartulyari, A.; Maier, M. E., Science of Synthesis Knowledge Updates, (2010) 3, 110. 摘要:MacMillan, D. W. C.; Watson, A. J. B., Science of Synthesis: Asymmetric Organocatalysis, (2012) 1, 363. 摘要:Littke, A., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 204.