专利号:US-2022081407-A1 优先权日:2020-09-11 标题 :Methods of preparing substituted indanes 发明人:STENGEL PETER J; XU RUI; SPENCER STACEY RENEE 权利人:PELOTON THERAPEUTICS INC 摘要:This application discloses methods for the synthesis of substituted indane analogs that modulate HIF-2α activity, as well as key intermediates produced thereby. The synthesis of 3-(((1S,2S,3R)-2,3-difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1H-inden-4-yl)oxy)-5-fluorobenzonitrile was exemplified.
专利号:US-5817827-A 优先权日:1995-11-21 标题:Method for the dehydration of amides to nitriles 发明人:BONRATH WERNER; PAULING HORST 权利人:HOFFMANN LA ROCHE 摘要:The present invention relates to a process for the dehydration of amides to nitrites which comprises carrying out the dehydration in the presence of an adduct of sulphur trioxide and an amine as the dehydrating reagent in a basic reaction mixture. Thereby, for example, aliphatic, aromatic and heteroaromatic amides are dehydrated to the corresponding nitrites, such as 5-carbamoyl-4-methyl-oxazole to 5-cyano-4-methyl-oxazole, a valuable intermediate in the synthesis of pyridoxine.
专利号:US-5254558-A 优先权日:1991-08-15 标 题:Substituted 1,3-diazines as leukocyte elastase inhibitors 发明人:BERNSTEIN PETER R; EDWARDS PHILIP D; THOMAS ROYSTON M; VEALE CHRIS A; WARNER PETER; WOLANIN DONALD J 权利人:ICI PLC 摘要:The present invention relates to certain novel substituted heterocycles which are 1-pyrimidinylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these substituted heterocycles, processes for preparing the substituted heterocycles, pharmaceutical compositions containing such substituted heterocycles and methods for their use.
专利号:BR-112016017679-B1 优先权日:2014-02-21 标题 :5-BENZYLISOQUINOLINE DERIVATIVE COMPOUNDS FOR THE TREATMENT OF CARDIOVASCULAR DISEASES, PROCESS FOR THE SYNTHESIS OF SUCH COMPOUNDS AND PHARMACEUTICAL COMPOSITION CONTAINING THEM
专利号:EP-1641453-B1 优先权日:2003-06-25 标题 :Product containing at least one phosphatase cdc25 inhibitor combined with at least one other anticancer agent 发明人:PREVOST GREGOIRE; BREZAK PANNETIER MARIE-CHRISTINE; DIOLEZ CHRISTIAN 权利人:IPSEN PHARMA 摘要:The invention relates to a product containing at least one phosphatase Cdc25 inhibitor combined with at least one other anticancer agent for simultaneous, separate or staggered therapeutic use during treatment for cancer. According to the invention, the other anticancer agent is preferably selected from: DNA base analogs such as 5-fluorouracil; inhibitors of type I and/or type II topoisomerases, such as camptothecin and the analogs thereof, doxorubicin or amsacrine; compounds interacting with the cellular spindle, for example, paclitaxel (Taxol); compounds acting on the cytoskeleton, such as vinblastine; inhibitors of the transduction of the signal passing via the heterotrimeric G proteins; prenyltransferase inhibitors, and especially farnesyltransferase inhibitors; cyclin-dependent kinase (CDKs) inhibitors; alkylating agents such as cisplatin; folic acid antagonists such as methotrexate; and inhibitors of DNA synthesis and cellular division, such as mitomycin C. The invention also relates to (1R)-1-[({(2R)-2-amino--3-[(8S)-8-(cyclohexylmethyl)-2-phenyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]--3-oxopropyl}dithio)methyl]-2-[(8S)-8-(cyclohexylmethyl)-2-phenyl--5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]-2-oxoethylamine, or the pharmaceutically acceptable salts thereof, that can be used as anticancer agents.
专利号:US-2008176865-A1 优先权日:2005-06-15 标 题:Substituted arylpyrazoles 发明人:BILLEN DENIS; BOYLE JESSICA; CRITCHER DOUGLAS JAMES; GETHIN DAVID MORRIS; HALL KIM THOMAS; KYNE GRAHAM MICHAEL 权利人:PFIZER LTD 摘要:This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.
[参考文献]: V K Rastogi, Et Al. 3,5-Difluorobenzonitrile: Ab Initio Calculations, Ftir And Raman Spectra. Spectrochim Acta A Mol Biomol Spectrosc. 2002 Jul;58(9):1987-2004.
合成参考文献
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