专利号:US-5424436-A 优先权日:1990-08-10 标题 :Processes for the synthesis of unsymmetrical secondary amines 发明人:GOE GERALD L; KEAY JAMES G; SCRIVEN ERIC F V; PRUNIER MICHAEL L; QUIMBY STEVEN J 权利人:REILLY IND INC 摘要:Imines are synthesized by the hydrogenation of pyridinecarbonitriles with amines in the presence of a rhodium-loaded catalyst. The resulting imines are stable and may be transiminated and then hydrogenated to form selected secondary amine products or may be hydrolyzed to aldehydes. n Further, a very useful class of unsymmetrical secondary amines represented by the formula RCH 2 NHAr (in which R is not aliphatic and Ar is aromatic and not attached to R), which has heretofore been accessible only with some difficulty, can be synthesized by processes herein disclosed utilizing the reductive intermolecular coupling of nitriles and primary aromatic amines.
专利号:EP-0548233-B1 优先权日:1990-08-10 标 题:Processes for the synthesis of imines, aldehydes, and unsymmetrical secondary amines 发明人:GOE GERALD; KEAY JAMES G; SCRIVEN ERIC F V; PRUNIER MICHAEL L; QUIMBY STEVEN J 权利人:REILLY IND INC 摘要:Imines are synthesized by the hydrogenation of pyridinecarbonitriles with amines in the presence of a rhodium-loaded catalyst. The resulting imines are stable and may be transiminated and then hydrogenated to form selected secondary amine products or may be hydrolyzed to aldehydes. Further, a very useful class of unsymmetrical secondary amines represented by the formula RCH2NHAr (in which R is not aliphatic and Ar is aromatic and not attached to R), which has heretofore been accessible only with some difficulty, can be synthesized by processes herein disclosed utilizing the reductive intermolecular coupling of nitriles and primary aromatic amines.
专利号:US-8981092-B2 优先权日:2008-09-19 标题 :Substituted 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-ones as modulators of protein kinase activity 发明人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO 权利人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO; NERVIANO MEDICAL SCIENCES SRL 摘要:Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, n nor pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
专利号:US-7468375-B2 优先权日:2004-04-26 标题:Inhibitors of the HIV integrase enzyme 发明人:DRESS KLAUS RUPRECHT; HU QIYUE; JOHNSON TED WILLIAM; PLEWE MICHAEL BRUNO; TANIS STEVEN PAUL; WANG HAI; YANG ANLE; YIN CHUNFENG; ZHANG JUNHU 权利人:PFIZER 摘要:The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIVâ€?) integrase enzyme.
专利号:US-4963572-A 优先权日:1987-08-12 标题:N-pyridyl methyl-N-'-cyanoisothiourea compounds useful in controlling insect pests 发明人:GSELL LAURENZ 权利人:CIBA GEIGY CORP 摘要:Novel substituted N-pyridylmethyl-N'-cyanoisothioureas of formula wherein R is C1-C4alkyl, cyclopropyl or benzyl; R1 is C1-C4alkyl or cyclopropyl; X is halogen; and n is the integer 0, 1, 2 or 3. Processes for the preparation of these compounds, the corresponding starting materials and intermediates and the use of the novel compounds in pest control, especially for controlling insects and representatives of the order Acarina, especially insect pests in rice crops, and as starting materials for the synthesis of novel pesticidal compositions are described.
专利号:EP-0548233-A1 优先权日:1990-08-10 标 题:METHODS OF SYNTHESIS OF IMINES, ALDEHYDES AND NON-SYMMETRIC SECONDARY AMINES.
参考文献:10.1177/2472555219873068 摘要:Lee OW, Austin S, Gamma M, Cheff DM, Lee TD, Wilson KM, Johnson J, Travers J, Braisted JC, Guha R, Klumpp-Thomas C, Shen M, Hall MD. Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. SLAS Discov. 2020 Jan;25(1):9–20.