专利号:US-11325912-B2 优先权日:2019-05-09 标题 :Regio-selective synthesis of imidazo[1,2-a]pyrimidines 发明人:CLAGG KYLE BRADLEY PASCUAL; WHITE NICHOLAS ANDREW; ZHANG HAIMING; GOSSELIN FRANCIS; NACK WILLIAM; O'SHEA PAUL D 权利人:GENENTECH INC 摘要:A method of regio-selectively synthesizing an imidazo-pyrimidine compound of formulae (XXa) or (XXb)comprising a step of coupling a first compound of formula XX-P1a or XX-P1b with a second compound of formula XX-P2This annulation reaction between β-ethoxy acrylamides and phosphorylated aminoimidazoles to furnish imidazo[1,2-a]pyrimidin-amines relies on steering effects from endocyclic and exocyclic phosphorylated aminoimidazoles. The reaction furnishes either 2-amino or 4-amino constitutional isomers of imidazo[1,2-a]pyrimidines with good yields and ranges of 90:10-99:1 regio-selectivity. The reaction is useful in the synthesis of various tracer molecules used in the study of neurological conditions such as where R3 and R4 together with the imidazole ring atoms to which they are bonded form a phenyl ring and the products are substituted benzimidazopyrimidines. The reaction can be generalized to form imidazo[1,2-a]pyrimidines substituted at either of their 2- and 4-positions by alkoxy or thioalkyl groups.
专利号:US-11034646-B2 优先权日:2017-09-29 标 题:Method for the synthesis of unsymmetrical tertiary amines 发明人:BOUR CHRISTOPHE; VAYER MARIE JENNY JACQUELINE; GANDON VINCENT 权利人:UNIV PARIS SACLAY; CENTRE NAT RECH SCIENT 摘要:Disclosed is a new method for the synthesis of unsymmetrical tertiary amines using alcohol and an imine, and to new tertiary amines.
专利号:US-9856205-B2 优先权日:2011-09-28 标 题:Method for the selective production of N-methyl-para-anisidine 发明人:IVANOV YURIY ALEXANDROVICH; BELIAKOV NIKOLAY GRIGORIEVICH 权利人:IVANOV YURIY ALEXANDROVICH; FROLOV ALEXANDER YURIEVICH; BELIAKOV NIKOLAY GRIGORIEVICH; IFOTOP LLC 摘要:The invention “Method for selective synthesis of N-methyl-para-anisidineâ€? relates to chemical technology processes, namely to catalytic alkylation of aromatic amines and nitro compounds. n The invention relates to the method for synthesis of N-methyl-para-anisidine (N-methyl-para-methoxyaniline; N-methyl-para-amino anisole) from para-anisidine (para-amino anisole; para-methoxyaniline) or para-nitro anisole (1-methoxy-4-nitrobenzene) and methanol in the presence of hydrogen or without hydrogen on heterogeneous catalyst. n Proposed method permits to use existing process plants used for obtaining aniline and 14-methylaniline. n The invention purpose is to provide the possibility to produce N-methyl-para-anisidine with purity at least 98% and high output that allows arrangement of highly profitable industry-scale manufacturing process.
专利号:US-9040480-B2 优先权日:2006-02-08 标题:Synthesis of glucagon-like peptide 发明人:WERBITZKY OLEG; VARRAY STÉPHANE; GIRAUD MATTHIEU; MEININGHAUS CARSTEN 权利人:LONZA AG 摘要:A new method of synthesizing GLP-1 peptide is devised.
专利号:US-4990625-A 优先权日:1982-08-31 标题 :Process for synthesis of N,N-disubstituted hydrazone 发明人:ARITA TETSUO; MABUCHI MINORU; UMEHARA SHOJI; SAKAI KIYOSHI 权利人:CANON KK 摘要:A process for synthesizing an N,N-disubstituted hydrazone comprises carrying out nitrozation by adding an aqueous solution of sodium nitrite to a solution having one part by weight of an N,N-disubstituted amine dissolved in 3 to 30 parts by weight of an organic acid, then reducing the nitrozated product to an N,N-disubstituted hydrazine by adding a reducing agent to the mixture containing the nitrozated product, and thereafter adding to the mixture containing the N,N-disubstituted hydrazine a carbonyl compound of the formula: ##STR1## wherein A represents an aromatic hydrocarbon group or an aromatic heterocyclic group which may have a substituent, B represents a hydrogen atom, an alkyl group, an aryl group or an aromatic heterocyclic group, which may have a substituent, thereby performing condensation of the N,N-disubstituted hydrazine with the carbonyl compound.
专利号:US-9676783-B2 优先权日:2008-10-22 标 题:Method of treatment using substituted pyrazolo[1,5-A] pyrimidine compounds 发明人:HAAS JULIA; ANDREWS STEVEN W; JIANG YUTONG; ZHANG GAN 权利人:ARRAY BIOPHARMA INC 摘要:Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
[参考文献]: Takuto Nagano, Et Al. Additive Effects Of Amines On Asymmetric Hydrogenation Of Quinoxalines Catalyzed By Chiral Iridium Complexes. Chemistry. 2012 Sep 10;18(37):11578-92.
合成参考文献
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