专利号:WO-2013164856-A1 优先权日:2012-05-04 标题 :A process for preparing intermediates of 10-propargyl-10-deazaaminopterin (pralatrexate) synthesis and the intermediates thereof 发明人:ALLA RAMA RAO VENKATA; RAMARAO CHANDRASHEKAR; MICHEL PATRICK THOMAS; NITLIKAR LAKSHMIKANT HANUMANTHRAO; KALAM BHUPATHI REDDY; DUDUKA RAMPRASAD 权利人:AVRA LAB PRIVATE LTD; ALLA RAMA RAO VENKATA; RAMARAO CHANDRASHEKAR; MICHEL PATRICK THOMAS; NITLIKAR LAKSHMIKANT HANUMANTHRAO; KALAM BHUPATHI REDDY; DUDUKA RAMPRASAD 摘要:A process for preparation of 4-(1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl)benzoic acid and other key intermediates in synthesis of 10-propargyl-10-deazaaminopterin (Pralatrexate) and the intermediates thereof. The 10-propargyl-10-deazaaminopterin (Pralatrexate) is obtained by peptide formation and ester hydrolysis of the intermediate compound 4-(1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl)benzoic acid by methods known in the art.
专利号:US-10799441-B2 优先权日:2011-06-06 标题:Skin treatments containing pyrroloquinoline quinone (PQQ) esters and methods of preparation and use thereof 发明人:LEWIS II JOSEPH ABERNATHY; DINARDO JOSEPH C 权利人:LEWIS II JOSEPH ABERNATHY; DINARDO JOSEPH C; PCR TECH HOLDINGS LC 摘要:The present invention relates to cosmetic or dermatological compositions containing PQQ or its esters, methods of treating or promoting skin changes by topical application of these compositions, and methods of synthesis of PQQ esters. The PQQ ester-containing compositions of the present invention are unexpectedly effective in treating skin, particularly with respect to skin tolerance. When included in a topical composition, the PQQ esters of the present invention have an antioxidant effect that is useful in treating a skin change.
专利号:US-5654441-A 优先权日:1995-09-14 标 题 :Synthesis of 1,3-oxathiolane sulfoxide compounds 发明人:MCPHEE DEREK JAMES 权利人:UNIROYAL CHEMICAL LTD 摘要:A process for the production of a 1,3-oxathiolane sulfoxide of the formula ##STR1## wherein X is an amino group of the formula --NHR, wherein R is hydrogen, phenyl, C 1 -C 8 alkyl, C 3 -C 6 cycloalkyl, nitrophenyl, (C 1 -C 4 alkoxy)phenyl, furfuryl, halophenyl, tolyl, napthyl, biphenyl or hydroxyphenyl; or X is an alkoxy group of the formula --OR 1 wherein R is C 1 -C 6 alkyl, n which process comprises oxidizing a 1,3-oxathiolane of the formula ##STR2## wherein X is as defined above, in the presence of an effective amount of aqueous hydrogen peroxide and a sterically-hindered organoselenium compound of the formula ##STR3## wherein R 2 is aryl, mono-, di- or tri-substituted with C 1 -C 3 alkyl, n to the produce the 1,3-oxathiolane sulfoxide. This process stereoselectively produces the cis stereoisomer of the 1,3-oxathiolane sulfoxide. Additionally, there is disclosed a novel method for the preparation of 5,6-dihydro-2-methyl-1,4-oxathiin compounds using this process.
专利号:US-4286091-A 优先权日:1980-05-19 标 题:Synthesis of pyridazinone pharmaceutical intermediates using diketene reactant 发明人:BIMBER RUSSELL M; BUCHMAN RUSSELL; DEPOMPEI MICHAEL F; POWERS LARRY J 权利人:DIAMOND SHAMROCK CORP 摘要:Valuable pyridazinone intermediates to pharmaceutically useful compounds can be prepared in surprisingly high yields by the reaction of the corresponding monohydrazone with diketene, preferably in the presence of a basic catalyst. In an especially preferred embodiment, p,p'-dichlorobenzil monohydrazone and diketene are reacted in a xylene solvent in the presence of triethylamine to afford 4-acetyl-5,6-bis(p-chlorophenyl)-2H-pyridazin-3-one, which can then be reacted with ethylene carbonate in the presence of potassium carbonate to afford the antihypertensive agent, 4-acetyl-5,6-bis(p-chlorophenyl)-2-(2'-hydroxyethyl)-2H-pyridazine-3-one.
专利号:US-4281125-A 优先权日:1980-05-15 标题:Quinoline catalyzed synthesis of pyridazinone pharmaceutical intermediates 发明人:DEPOMPEI MICHAEL F; HLYNSKY ALEX 权利人:DIAMOND SHAMROCK CORP 摘要:Valuable pyridazinone intermediates to pharmaceutically useful compounds can be prepared in surprisingly high yields by the quinoline catalyzed reaction of the corresponding monohydrazone with an appropriately substituted acetic acid ester. In an especially preferred embodiment, p,p'-dichlorobenzil monohydrazone and methyl acetoacetate are reacted in a xylene solvent in the presence of quinoline to afford 4-acetyl-5,6-bis(p-chlorophenyl)-2H-pyridazin-3-one, which can then be reacted with ethylene carbonate in the presence of potassium carbonate to afford the antihypertensive agent, 4-acetyl-5,6-bis(p-chlorophenyl)-2-(2'-hydroxyethyl)-2H-pyridazin-3-one.
专利号:US-4104140-A 优先权日:1972-10-05 标题:Process for the electrochemical synthesis of organic metal compounds 发明人:EISENBACH WILHELM; LEHMKUHL HERBERT; WILKE GUNTHER 权利人:STUDIENGESELLSCHAFT KOHLE MBH 摘要:Process for reacting an H-acidic organic compound, in which the acidic H-atom is bonded to the organic radical by an oxygen or a sulphur atom, e.g. an alcohol, with a metal having a standard potential which is more positive than -1.66 volts and which at most incompletely reacts with the H-acidic compound under current-free conditions, e.g. Ni, Co, Fe, Mn, Sb, Cu, or Au. The H-acidic compound or a solution thereof is a polar solvent is made conducting by addition of a soluble salt of chlorine, bromine or iodine, and is electrolyzed at a temperature of up to 150° C, using said metal as the anode, for production of the alcoholate.