专利号:US-4062865-A 优先权日:1974-04-05 标 题:Process for the synthesis of substituted indolenines 发明人:MOGGI PIETRO ANTONIO 权利人:SNAM PROGETTI 摘要:A process for the preparation of substituted indolenines of the formula: ##STR1## wherein R is hydrogen, alkyl, aryl or cycloalkyl, halogen, or a functional group selected from among cyano, hydroxyl, alkoxy, nitro or sulphonic groups, and wherein R 1 , R 2 and R 3 are the same, or different, and are selected from alkyl, aryl or cycloalkyl radicals, comprising reacting in the presence of an organic solvent an aromatic amine of the formula: ##STR2## with a tertiary hydroxyketone of the formula: ##STR3## wherein R, R 1 , R 2 and R 3 have the same meanings as defined above, in the presence of a catalyst selected from mineral acids, organic acids, Lewis acids or ionic exchange resins in acid form, and wherein said aromatic amine is slightly in excess, to form first an imine of the formula: ##STR4## under reaction conditions wherein the solvent is removed by azeotropic distillation, and thereafter continuing the reaction to remove water and cyclizing to the desired indolenines. In a preferred embodiment, 2,3,3-trimethylindolenine is prepared by reacting an excess of aniline with 3-methyl-3-hydroxybutan-2-one in the presence of ZnCl 2 as catalyst utilizing benzene as solvent. The substituted indolenines obtained are useful in production of dyes and other compounds useful in the dyeing and photographic industries.
专利号:US-8143437-B2 优先权日:2002-02-19 标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof 发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X 权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC 摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
专利号:WO-03080621-A1 优先权日:2002-03-19 标题:Process and intermediates to substituted imidazopyrimidines 发明人:LI WENJIE; CAI DONGWEI; HOERRNER R SCOTT; JENSEN MARK S; LARSEN ROBERT D; PETASIS NICOS A 权利人:MERCK & CO INC; LI WENJIE; CAI DONGWEI; HOERRNER R SCOTT; JENSEN MARK S; LARSEN ROBERT D; PETASIS NICOS A 摘要:A novel process is provided for the preparation of imidazo[1,2-α]pyrimidines which are substituted at the 3-position with a substituted chlorophenyl group. Such compounds are useful in the synthesis of GABAA receptor ligands for the treatment of deleterious mental disorders. Also provided are intermediates obtained from the process useful in the synthesis of GABAA receptor ligands.
专利号:US-10017435-B2 优先权日:2014-06-10 标 题 :Process for the preparation of a phenylindan compound 发明人:NORCINI GABRIELE; CASIRAGHI ANGELO; MENEGUZZO ENZO; FLORIDI GIOVANNI; LI BASSI GIUSEPPE 权利人:IGM RESINS ITALIA SRL; IGH RESINS ITALIA S R L 摘要:The present invention refers to a process for producing 5-[4-(2-hydroxy-2-methyl)-1-oxo-prop-1-yl]-3-[4-(2-hydroxy-2-methyl)-1-oxo-prop-1-yl-phenyl]-2,3-dihydro-1,1,3-trimethyl-1H-indene (dimer isomer 5) that comprises the synthesis from cumene and dimerization of 2-methyl-1-(4-(prop-1-en-2-yl)phenyl)propan-1-one in the presence of acid catalysts.
专利号:US-2005239725-A1 优先权日:2002-02-19 标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
专利号:US-6232467-B1 优先权日:1996-06-28 标 题:Method for the synthesis of amines and amino acids with organoboron derivatives 发明人:PETASIS NICOS A; ZAVIALOV ILIA A 权利人:UNIV SOUTHERN CALIFORNIA 摘要:Amines and amino acids are prepared by reacting an amine, a carbonyl derivative, and an organoboron compound under mild conditions.
摘要:Gagnon, A.; Benoit, E.; Le Roch, A., Science of Synthesis Knowledge Updates, (2018) 4, 69. 摘要:Chiang, P.-C.; Bode, J. W., Science of Synthesis: Asymmetric Organocatalysis, (2012) 1, 663.