2,2-Dimethyl-5-({[4-(Propan-2-yl)Phenyl]Amino}Methylidene)-1,3-Dioxane-4,6-Dione 以 二苯醚 用作溶剂,化学反应 0.08H,反应生成6-异丙基喹啉 参考文献:Synthesis Of Ring-Substituted 4-Aminoquinolines And Evaluation Of Their Antimalarial Activities 标题:Synthesis Of Ring-Substituted 4-Aminoquinolines And Evaluation Of Their Antimalarial Activities 摘要:A Simple Two-Step Synthesis Method Was Used To Make 51 B-Ring-Substituted 4-Hydroxyquinolines Allowing Analysis Of The Effect Of Ring Substitutions On Inhibition Of Growth Of Chloroquine Sensitive And Resistant Strains Of Plasmodium Falciparum,The Dominant Cause Of Malaria Morbidity. Substituted Quinoline Rings Other Than The 7-Chloroquinoline Ring Found In Chloroquine Were Found To Have Significant Activity Against The Drug-Resistant Strain Of P. Falciparum W2. (C) 2004 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmcl.2004.12.037
专利号:US-9982005-B2 优先权日:2013-04-04 标 题 :Macrolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.
专利号:US-6930113-B2 优先权日:1996-11-01 标题 :Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use 发明人:GARVEY DAVID S; DE TEJADA INIGO SAENZ; EARL RICHARD A; KHANAPURE SUBHASH P 权利人:NITROMED INC 摘要:The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing diseases induced by the increased metabolism of cyclic guanosine 3′,5′-monophosphate (cGMP), such as hypertension, pulmonary hypertension, congestive heart failure, renal failure, myocardial infraction, stable, unstable and variant (Prinzmetal) angina, atherosclerosis, cardiac edema, renal insufficiency, nephrotic edema, hepatic edema, stroke, asthma, bronchitis, chronic obstructive pulmonary disease (COPD), cystic fibrosis, dementia, immunodeficiency, premature labor, dysmenorrhoea, benign prostatic hyperplasis (BPH), bladder outlet obstruction, incontinence, conditions of reduced blood vessel patency, e.g., postpercutaneous transluminal coronary angioplasty (post-PTCA), peripheral vascular disease, allergic rhinitis, glucoma, and diseases characterized by disorders of gut motility, e.g., irritable bowel syndrome (IBS).
专利号:US-2004152897-A1 优先权日:2002-09-13 标 题 :Synthesis of indolizines 发明人:SUN LIJUN; KOYA KEIZO; XIA ZHI-QIANG; PRZEWLOKA TERESA; ZHANG SHIJIE; ONO MITSUNORI 权利人:SYNTA PHARMACEUTICALS CORP 摘要:Disclosed are methods of preparing substituted indolizines represented by the following formula: n n n comprising reacting a substrate represented by the following formula: n n n with either the cyclization reagent of the following formula: n n n or, a reagent prepared by reacting the compound represented the formula below with an alkylating agent: n n n The variables in the above formulas are defined herein.
专利号:US-2003158184-A1 优先权日:2001-12-21 标 题 :Nitrosated and nitrosylated phosphodiesterase inhibitor compounds, compositions and their uses 发明人:GARVEY DAVID S; DE TEJADA INIGO SAENZ 摘要:The invention provides methods for treating female sexual dysfunctions by administering to a female individual a therapeutically effective amount of at least one compound that donates, transfers or release nitrogen monoxide, that induces the production of endogenous endothelium-derived relaxing factor, that stimulates endogenous synthesis of nitrogen monoxide, or that is a substrate for nitric oxide synthase. The methods may further comprise administering a therapeutically effective amount of a phosphodiesterase inhibitor and/or a nitrosated and/or nitrosylated phosphodiesterase inhibitor.
专利号:WO-2023072969-A1 优先权日:2021-10-26 标题 :Imidazolone derivatives as inhibitors of protein kinases in particular dyrk1a, clk1 and/or clk4 发明人:DEAU EMMANUEL; GEORGE PASCAL; MEIJER LAURENT; MIEGE FRÉDÉRIC; ARCHAMBAUD SYLVIE 权利人:PERHA PHARMACEUTICALS 摘要:The present invention relates to a compound of formula (I) wherein A, B, C, D and E are selected from the group consisting of =CH- and -N=, R 2 is selected from a hydrogen atom, a (C 1 -C 4 )alkyl group and a (C 3 -C 6 )cycloalkyl group, R 1 represents a (C 4 -C 6 )alkyl group, a (C 3 -C 8 )cycloalkyl group, a bridged (C 6 -C 10 )cycloalkyl group, a fused phenyl group, a substituted phenyl group, a R'-L- group, wherein L is either a single bond or a (C 1 -C 3 )alkanediyl group, and R' represents, a (C 3 -C 8 )heterocycloalkyl group, or a (C 3 -C 8 )heteroaryl group, or a R'-L- group wherein L is a (C 1 -C 3 )alkanediyl group, and R' is a an optionally substituted phenyl group or any of its pharmaceutically acceptable salt. The present invention further relates to a composition comprising a compound of formula (I) and a process for manufacturing said compound as well as its synthesis intermediates. It also relates to said compound for use as a medicament, in particular in the treatment and/or prevention of cognitive deficits and neuroinflammation associated with Down syndrome, Alzheimer's disease, dementia and/or tauopathies; Parkinson's disease; CDKL5 Deficiency Disorder; Phelan-McDermid syndrome; autism; type 1 and type 2 diabetes; abnormal folate and methionine metabolism; tendinopathy and osteoarthritis; Duchenne muscular dystrophy; several cancers; neuroinflammation, anemia, infections and for regulating body temperature.
专利号:WO-2017004172-A1 优先权日:2015-06-29 标题:Total synthesis of shishijimicin a and analogs thereof
参考标题:Assembly Of Diversely Substituted Quinolines Via Aerobic Oxidative Aromatization From Simple Alcohols And Anilines 作者:Jixing Li,Jinlong Zhang,Huameng Yang,Gaoxi Jiang |发布日期:2017.3.17 摘要:Acid Catalytic System Has Been Established, Providing A Direct Approach For The Preparation Of Diverse Substituted Quinoline Derivatives In High Yields With Wide Functional Group Tolerance. Practically, The Protocol Can Be Easily Scaled Up To Gram-Scale And Was Utilized In The Concise Formal Synthesis Of A Promising Herbicide Candidate.
合成参考文献
摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 417.