专利号:US-4871873-A 优先权日:1988-03-18 标 题:Process for synthesis of arylglyoxal arylimines 发明人:DESMOND RICHARD; MILLS SANDER G; VOLANTE RALPH P; SHINKAI ICHIRO 权利人:MERCK & CO INC 摘要:A process for producing arylglyoxal arylimine intermediates, by the DMSO/HBr oxidation of arylmethylketones. The imine compounds are intermediates in the synthesis of carbapenem antibiotics, i.e. imipenem.
专利号:EP-1383732-B1 优先权日:2001-05-04 标题:Labelling reagents, method for synthesis of said reagents and methods for detecting biological molecules 发明人:BOURGET CECILE; LHOMME JEAN; LAAYOUN ALI; KOTERA MITSUHARU; TREVISIOL EMMANUELLE; MENOU LIONEL; BERNAL MENDEZ ELOY 权利人:BIO MERIEUX; UNIV GRENOBLE 1; CENTRE NAT RECH SCIENT 摘要:The invention concerns a temperature-stable labelling reagent of formula (I), wherein: R<1> represents H or an alkyl, aryl or substituted aryl group; R<2> represents a detectable marker or at least two detectable markers linked together by at least a multimeric structure; L is a linking arm comprising a linear catemer concatenation of at least two covalent bonds; and n is an integer equal to 0 or 1; R<3> and R<4> represent, independently of each other: H, NO2, Cl, Br, F, I, R<2>-(L)n-Y-X-, OR, SR, NR2, R, NHCOR, CONHR, COOR with R = alkyl or aryl, A is a linking arm comprising at least a double bond enabling the conjugation of the diazo function with the aromatic cycle; and u is a whole number between 0 and 2, preferably between 0 and 1; and -Y-X- represents -CONH-, -NHCO-, -CH2O-, -CH2S-. The invention also concerns a method for the synthesis of said markers and uses for labelling biological molecules, in particular nucleic acids, with a labelling reagent bearing the diazomethyl function. The invention is particularly applicable in the field of diagnosis.
专利号:US-11078163-B2 优先权日:2014-01-24 标 题 :Processes for the synthesis of substituted urea compounds 发明人:RUSSO DOMENICO; WAHNON JORGE BRUNO REIS; MATON WILLIAM; ESZENYI TIBOR 权利人:BIAL PORTELA & CA SA; BIAL PORTELA & Cª S A 摘要:The present invention concerns a process for preparing a compound having the Formula A; or a pharmaceutically acceptable salt or derivative thereof, or for preparing a substituted urea compound of Formula IIa, or a pharmaceutically acceptable salt or ester thereof, the process comprising the reaction of an imidazolyl intermediate of Formula IIa′ with a carbamoyl halide of the formula: R1R2NC(â•?O)Hal, wherein Hal represents Cl, F, I or Br, wherein the intermediate of Formula IIa′ is prepared by oxidation of the derivative of R5 and R6, R6-C(â•?O)CH2R5 to form a glyoxal intermediate R6-C(â•?O)(Câ•?O)R5, which is subjected to treatment with ammonium hydroxide and an aldehyde R8CHO to provide the intermediate of Formula IIa′ and wherein the compound substituents are as defined herein.
专利号:US-9150497-B2 优先权日:2011-10-14 标题 :Continuous two step flow synthesis of M-amino acetophenone 发明人:KULKARNI AMOL ARVIND; JOSHI RAMESH ANNA; JOSHI ROHINI RAMESH 权利人:COUNCIL SCIENT IND RES 摘要:Disclosed herein is a continuous tubular reactor based conversion of acetophenones to amino substituted acetophenones wherein the nitration is carried out at −10 to 10° C. followed by reduction to m-nitrophenone resulting in uniform output of product, said process comprising the steps of: a) Nitrating acetophenone with nitrating agent (nitration mixture or fuming nitric acid) at −10 to 10° C.; b) Isolating m-nitro acetophenone from a mixture of o and m-nitro acetophenone and c) Reducing the m-nitro to obtain m-amino acetophenone.
专利号:JP-6777542-B2 优先权日:2014-01-24 标题:Process for the synthesis of substituted urea compounds
专利号:CA-2444918-C 优先权日:2001-05-04 标 题:Labelling reagents, method for synthesis of said reagents and methods for detecting biological molecules