(2E)-3-(二甲基氨基)-2-甲酰基丙烯腈置于盐酸,肼体系中,用 乙醇 用作溶剂,化学反应 1.0H,以55%的收率获得1H-吡唑-4-腈 参考文献:Cyanoacetaldehyde New Synthetic Applications Of An Old Compound Syntheses With Nitriles,Xci 标题:Cyanoacetaldehyde New Synthetic Applications Of An Old Compound Syntheses With Nitriles,Xci 摘要:Various Reactions Of Cyanoacetaldehyde (1),Freshly Prepared By Ozonization Of (E)-1,4-Dicyano-2-Butene Or Allylcyanide,Are Described. Thus,Conversion Of 1 With Anilines Gave Beta-Phenylaminoacrylonitriles 2A-E. Reaction Of 1 With Hydrazines Led To The Corresponding Hydrazones 3A-E,Which Could Be Cyclized Under Alkaline Conditions To 5-Aminopyrazoles 4A-D. An Aldol-Type Condensation Product 5A Could Be Obtained By Reaction Of 1 With Sodiumphenoxide. Treatment Of 1 With Dimethylformamide-Dimethylacetal Led To The Formation Of (E)-3-Dimethylamino-2-Formylpropenenitrile (6),A Very Useful Synthon In Synthetic Chemistry. For The Determination Of The Structure Of 6 The Method Of Steady State Differential Noes Was Used. Reaction Of 6 With Hydrazines Gave 1-Substituted-4-Cyanopyrazoles 7A-K. Doi:10.1007/bf00808679
专利号:US-5144015-A 优先权日:1990-12-21 标 题 :Synthesis of pyrazole dyes 发明人:CHAPMAN DEREK D 权利人:EASTMAN KODAK CO 摘要:A process for preparing a 1-alkyl-3-secondary or tertiary alkyl-4-cyano-pyrazol-5-yl azo dye or a 1-alkyl-3-aryl-4-cyano-pyrazol-5-yl azo dye comprising: n a) reacting a 3-secondary or tertiary alkyl-4-cyano-5-amino pyrazole or a 3-aryl-4-cyano-5-amino pyrazole with a diazotizing reagent to form a pyrazol-5-yl diazonium salt; n b) allowing said diazonium salt to react with an aromatic coupling component to form a 3-secondary or tertiary alkyl-4-cyano-pyrazol-5-yl azo dye or a 3-aryl-4-cyano-pyrazol-5-yl azo dye; and n c) reacting the product of step b) with an aklylating agent in the presence of a base to form a 1-alkyl-3-secondary or tertiary alkyl-4-cyano-pyrazol-5-yl azo dye or a 1-alkyl-3-aryl-4-cyano-pyrazol-5-yl azo dye.
专利号:US-7772394-B2 优先权日:2003-09-04 标题 :Zaleplon synthesis 发明人:KANKAN RAJENDRA NARAYANRAO; RAO DHARMARAJ RAMACHANDRA 权利人:CIPLA LTD 摘要:A process for making zaleplon comprising alkylating 3-[3-(dimethylamino)-1-oxo-2-propenyl]-phenyl]-acetamide with ethyl iodide in the presence of an alkali metal hydroxide or alkoxide selected from sodium hydroxide, potassium hydroxide, sodium methoxide, sodium tert-butoxide or potassium tert-butoxide in an aprotic solvent to give N-ethyl-[3-[3-(dimethylamino)-1-oxo-2-propenyl]-phenyl]-acetamide, condensing N-ethyl-[3-[3-(dimethylamino)-1-oxo-2-propenyl]-phenyl]-acetamide and 3-amino-4-cyanopyrazole, and isolating zaleplon from the reaction. Preferably, the condensing is done in the presence of (a) a water immiscible organic acid; (b) a cation exchange resin; or (c) a water miscible organic acid in water or in a C-1 to C-4 alcohol or in a mixture of water and a C-1 to C-4 alcohol.
专利号:BR-112016002339-B1 优先权日:2013-08-09 标 题:COMPOUND, METHODS FOR SYNTHESIS OF A COMPOUND AND FOR CONTROL OF UNDESIRABLE PLANTS, AND, COMPOSITION OF HERBICIDE
专利号:US-11091490-B2 优先权日:2016-11-30 标 题:3-amino-1,5-dihydro-pyrazolo[3,4-d]pyrimidin-4-ones as cyclin dependent kinase inhibitors 发明人:WUNDERLECH WINFRIED; HUBER LUKAS A; LEBAN JOHANN JAKOB; PATÓ JÃ?NOS; ÖRFI LÃ?SZLÓ; FRIGYES WÃ?CZEK; BÃ?NHEGYI PÉTER; SÃ?POS ANNA; SZÃ?NTAI-KIS CSABA 权利人:ONCOTYROL CENTER FOR PERSONALIZED CANCER MEDICINE GMBH; VICHEM CHEMIE KUTATO KORLATOLT FELELOESSEGUE TARSASAG; MEDIZINISCHE UNIV INNSBRUCK 摘要:The present invention relates to 3-amino-pyrazolo[3,4-d]pyrimidin-4-ones, such as for example, N-{4-[1-(2,6-dichloro-4-sulfamoyl-phenyl)-3-dimethylamino-4-oxo-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-ylmethyl]-phenyl}-2-diethylamino-acetamide, particularly useful as cyclin dependent kinase (CDK) inhibitors, pharmaceutical compositions comprising the same and the use thereof in particular in the prophylaxis and/or treatment of cancer and other proliferative diseases. Furthermore, the present invention relates to processes for the synthesis of said 3-aminopyrazolo[3,4d]pyrimidin-4-ones and intermediates to be used in the processes of the present invention.
专利号:US-6518266-B1 优先权日:1999-07-22 标题:1- Aryl-3-thioalkyl pyrazoles, the synthesis thereof and the use thereof as insecticides 发明人:DHANOA DALJIT S; DOLLER DARIO; MEEGALLA SANATH; SOLL RICHARD M; WISNEWSKI NANCY; SILVER GARY; STINCHCOMB DAN T; SEWARD R LEE; AGRAFIOTIS DIMITRIS; SHA DEYOU 权利人:DIMENSIONAL PHARMACEUTICALS 3; HESKA CORP 摘要:The present invention is directed to novel pyrazole derivatives and their use as pesticidal agents. The pyrazole derivatives have Formula I:or a salt thereof, whereR1 represents R5O, R5SO2, R5SO or R5S in which R5 is as defined herein;X is halo, cyano, C1-6 alkoxycarbonyl, C2-6 alkynyl, optionally substituted C6-14 aryl or an optionally substituted 5- to 7-membered heteroaromatic ring linked to thiazole via a carbon-carbon bond;R2 is hydrogen, amino, chloro, bromo, iodo, cyano, C1-6 alkoxy, C1-6 alkyl or C6-10 aryl; andR3-R7 each represent hydrogen, halogen, straight- or branched-chain C1-4 alkyl or C1-4 alkoxy, either of which is unsubstituted or substituted by one or more halogen atoms, straight- or branched-chain C1-4 alkylthio or C1-4 alkylsulphinyl, either of which is substituted by one or more halogen atoms, nitro, cyano, or straight- or branched-chain C1-4 alkylsulphonyl group which is unsubstituted or substituted by one or more halogen atoms.
专利号:US-4093812-A 优先权日:1975-03-25 标 题:(Nitrofuryl)pyrazoles, their synthesis and use, and compositions containing them 发明人:RAINER GEORG 权利人:BYK GULDEN LOMBERG CHEM FAB 摘要:3-(5-Nitro-2-furyl)pyrazoles unsubstituted in the 5-position and 5-(5-nitro-2-furyl)pyrazoles unsubstituted in the 3-position are antimicrobials and disinfectants. The compounds are structurally represented by one of the formulae: ##STR1## wherein A is --CHO, --CN, --COOH, a protected or derived aldehyde group or a protected or derived carboxylic acid group; n B is 5-nitro-2-furyl; n R 1 is --H, substituted or unsubstituted hydrocarbyl (saturated or unsaturated; acyclic, alicyclic or aromatic; or araliphatic); substituted or unsubstituted (cycloaliphatic or aromatic) heterocyclic or acyl (carboxylic or carbonic acid); n R 2 is --H; and n n is a positive whole number of at most 2.
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025). 摘要:Yerien, D. E.; Barata-Vallejo, S.; Postigo, A., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 9.