Alpha,4-二氯苯甲醛肟置于sodium Azide体系中,用 甲醇,乙腈 作为反应溶剂,化学反应 12.0H,反应生成 对氯苯甲腈 参考文献:Azide Oximes And 1-Hydroxytetrazoles 标题:Azide Oximes And 1-Hydroxytetrazoles 摘要:Eleven Azide Oximes Were Prepared And Tested For Their Antiplatelet (In Vitro),Antithrombotic,And Blood Pressure Lowering Activities. Nine Of Them Inhibited The Aggregation Of Blood Platelets (Born Test,Inducer Collagen) With Ic50 Values Between 10 And 50 Microm. The Most Active Compounds I.E. Azido-4-Nitrophenylbenzaldoxime (2H) Had An Ic50 = 2 Microm. Nine Azide Oximes Exhibited Significant Antithrombotic Properties. The Most Active Compounds Were 2H And 2C (Azido-4-Methylphenylbenzaldoxime) With An Inhibition Of Thrombus Formation Above 20% In Arterioles After A Single P.O. Dose Of 60 Mg/kg. Both Compounds Lowered The Blood Pressure In Spontaneously Hypertensive Rats By 11% (2H) Or 5% (2C),Respectively. Seven Azide Oximes Were Rearranged To The Title Tetrazololes Which However Showed Smaller Antithrombotic Effects. In Separate In Vitro Experiments At 37 Degrees C It Could Be Demonstrated That Azide Oximes Release Nitric Oxide (Conversion Rate Approximately 10%.H-1) And Nitrosohydrogen (Conversion Rate Approximately 2%.H-1). This Makes It Appear Probable That The Above Effects Are Mediated By These Molecules. DOI:10.1002/1521-4184(20006)333:6<157::Aid-Ardp157>3.0.Co;2-C
专利号:US-5128485-A 优先权日:1990-12-17 标 题:Synthesis of 2-aryl-5-(trifluoromethyl)pyrroles useful as pesticidal agents and as intermediates for the preparation of said agents 发明人:KAMESWARAN VENKATARAMAN 权利人:AMERICAN CYANAMID CO 摘要:There is provided a synthesis of 2-aryl-5-(trifluoromethyl)pyrrole compounds of formula I via the condensation of a suitable enamine with an alpha -haloketone. 2
专利号:US-2015239796-A1 优先权日:2014-02-19 标题:One pot synthesis of 18f labeledtrifluoromethylated compounds with difluoro(iodo)methane 发明人:RüHL THOMAS; RISS PATRICK; RAFIQUE WAQAS 权利人:UNIV OSLO 摘要:The present invention relates to compositions and methods for the synthesis of 18 F labeled compounds. In particular, the present invention relates to a copper (I) mediated one pot method for 18 F-trifluoromethylation of aromatic- or heteroaromatic halides with difluoro(iodo)methane (e.g., for use at PET imaging agents).
专利号:US-5288868-A 优先权日:1992-02-13 标题:Process for the preparation of 2-hydroxy-4,6-diaryl-1,3,5-triazine 发明人:REINEHR DIETER; BACHER JEAN-PIERRE 权利人:CIBA GEIGY CORP 摘要:There is disclosed a process for the preparation of 2-hydroxy-4,6-diaryl-1,3,5-triazines by reacting an aromatic nitrile with an alkali metal amide and an alkyl haloformate, using an equimolar amount of each, which process is carried out as a one-pot synthesis. The triazine derivatives obtained by the process of this invention are used as intermediates for the synthesis of UV absorbers.
专利号:US-8252927-B2 优先权日:2008-07-22 标题:Synthesis of substituted 4-amino-pyrimidines 发明人:KARGE REINHARD; LETINOIS ULLA; SHIEFER GERHARD 权利人:KARGE REINHARD; LETINOIS ULLA; SHIEFER GERHARD; DSM IP ASSETS BV 摘要:The present invention is directed to a process for the manufacture of compounds of formula IV wherein R 1 is an amino protecting group, and R 2 is hydrogen or C 1-10 alkyl, comprising a) reacting a compound of formula Ia, wherein M + is a cation, preferably selected from the group consisting of Li + , Na+, K + , ½ Mg 2+ and ½ Zn 2+ , (formula 1 a ) with an ammonium salt NH 4 + X − , wherein X − is an anion, preferably selected from the group consisting of chloride, bromide, sulfate and acetate, in a solvent to a compound of formula II b) reacting a compound of formula II with a nitrile R 2 —CN in the presence of a base to a compound of formula IV. The present invention is further directed to compounds of formula II and their use for the manufacture of vitamin B 1 .
专利号:US-7705159-B2 优先权日:2005-07-06 标题:Process for the preparation of letrozole 发明人:MACDONALD PETER LINDSAY; BIGATTI ETTORE; ROSSETTO PIERLUIGI; HAREL ZVI 权利人:SICOR INC 摘要:The invention provides a high-yield process for the preparation of letrozole having a high purity, without the need for removal of the 4-[1-(1,3,4-triazolyl)methyl]benzonitrile impurity at the intermediate stage. The invention also provides a process for the synthesis of letrozole in which formation of the impurity 4-[1-(1,3,4-triazolyl)methyl]benzonitrile during the first stage is minimized. In the process, a 4-(halomethyl)benzonitrile is reacted with a salt of 1H-1,2,4-triazole, reducing the formation of the impurity. Preferably, the preparation is conducted as a one-pot process.
专利号:US-8212056-B2 优先权日:2008-06-30 标 题 :Ligands for transition-metals and methods of use 发明人:KWONG FUK YEE; SO CHAU MING 权利人:KWONG FUK YEE; SO CHAU MING; UNIV HONG KONG POLYTECHNIC 摘要:The present invention relates to indolyl phosphine ligands, and methods of making such ligands utilizing phenyl hydrazines and aryl ketones as the starting material. The present invention further includes uses of the ligands in the synthesis of pharmaceuticals, materials, and agriculture.
[参考文献]: Ondrej Kaplan, Et Al. Purification And Characterization Of A Nitrilase From Aspergillus Niger K10. Appl Microbiol Biotechnol. 2006 Dec;73(3):567-75.
合成参考文献
摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 587. 摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 562. 摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 596. 摘要:Alonso, D. A.; Nájera, C., Science of Synthesis, (2010) 45, 228. 摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 644.