专利号:US-6500955-B1 优先权日:2001-02-02 标 题:One pot synthesis of [2,8-Bis (trifluoromethyl)-4-quinolinyl]-2-pyridinylmethanone, a mefloquine intermediate 发明人:CHAWLA HARMANDER PAL SINGH; JOHAR PERMINDER SINGH; MITTAL ALKA; MEENA RAM AVTAR; NEGI VILLENDRA SINGH 权利人:NAT INST OF PHARMACEUTICAL EDU 摘要:The present invention provides a simple single step process for the preparation of [2,8-bis(trifluoromethyl)-4-quinolinyl]-2-pyridinylmethanone, comprising the step of condensing a halo-quinoline with an alpha-picolyl derivatives in the presence of a solvent, a base and a phase transfer catalyst at −10° C. to +90° C.
专利号:WO-2012107532-A1 优先权日:2011-02-11 标 题 :4-aminoalcoholquinoline derivatives, enantioselective synthesis methods and the use thereof 发明人:JONET ALEXIA; DASSONVILLE-KLIMPT ALEXANDRA; MULLIE CATHERINE; TAUDON NICOLAS; SONNET PASCAL 权利人:UNIV PICARDIE; JONET ALEXIA; DASSONVILLE-KLIMPT ALEXANDRA; MULLIE CATHERINE; TAUDON NICOLAS; SONNET PASCAL 摘要:The present invention is intended to provide new antimalarial compounds with a strong antimalarial activity as well as antibacterial activity with few neurological side effects and a new enantioselective pathway to mefloquine amino-analogs allowing the access of such compounds. The present invention relates to new 4 -aminoalcohol quinoline derivatives of formula (I), as well as the synthesis methods and the uses of such derivatives. In which Y is one selected from formulae (II) to (III). In which Z is selected from formulae (IV) to (VI), and wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and n are as defined in the claims.
专利号:US-3839346-A 优先权日:1972-12-18 标 题:N-substituted pyridone and general method for preparing pyridones 发明人:GADEKAR S 权利人:AFFILIATED MED RES 摘要:1. A PROCESS FOR THE SYNTHESIS OF PYRIDONES OF THE FORMULA 1-A,2-(O=),3-R3,4-R4,5-R5,6-R6-1,2-DIHYDROPYRIDINE WHEREIN A IS AN AROMATIC RADICAL SELECTED FROM THE GROUP CONSISTING OF PHENYL, TOLYL, CHLOROPHENYL, TRIFLUOROMETHYLPHENYL, NAPHTHYL, PYRIDYL, FURYL, THIENYL, THIAZOLYL, PYRIMIDYL, QUINOLYL, IMIDAZOLYL; UP TO TWO OF THE TERMS R3, R4, R5 AND R6 ARE INDIVIDUALLY EACH HYDROGEN OR ALKYL UP TO 6 CARBON ATOMS, ARYL OR SUBSTITUTED ARYL RADICALS WHICH CONSISTS ESSENTIALLY OF THE STEPS OF REACTING A PYRIDONE OF THE FORMULA 2-(O=),3-R3,4-R4,5-R5,6-R6-1,2-DIHYDROPYRIDINE, OR ITS TAUTOMER, 2-(HO-),3-R3,4-R4,5-R5,6-R6-PYRIDINE IN WHICH R3, R4, R5 AND R6 ARE SET FORTH ABOVE, WITH A HALOGENATED COMPOUND OF THE FORMULA AX, WHEREIN X IS EITHER CHLORINE, BROMINE OR IODINE, AT TEMPERATURES RANGING BETWEEN THE MELTING POINT AND BOILING POINT OF SAID HALOGENATED COMPOUND, IN THE PRESENCE OF AN ALKALI METAL CARBONATE AND FINELY DIVIDED METALLIC COPPER.
专利号:US-8633182-B2 优先权日:2012-05-30 标题:Indanyloxyphenylcyclopropanecarboxylic acids 发明人:HAMPRECHT DIETER; FRATTINI SARA; LINGARD IAIN; PETERS STEFAN 权利人:HAMPRECHT DIETER; FRATTINI SARA; LINGARD IAIN; PETERS STEFAN; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to compounds of general formula I, n nwherein the groups R 1 , R 2 , R 3 , m and n are defined as in claim 1 , which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
专利号:CN-1370777-A 优先权日:2001-02-02 标题:Improved single-reactor synthesis of [2,8-di(trifluoromethyl)-4-quinolyl]-2-pyridyl methyl ketone and methylfluoro quine
专利号:US-2002188129-A1 优先权日:2001-02-02 标题:One pot synthesis of [2, 8-bis (trifluoromethyl)-4- quinolinyl]2-pyridinylmethanone, a mefloquine intermediate