专利号:US-2009221834-A1 优先权日:2006-04-20 标题 :Synthesis of 5-Beta-Keto-1,2,4-Oxadiazoles and Conversion of 5-Beta-Keto-1,2,4 Oxadiazoles to N-Pyrazolyl Amidoximes 发明人:JENSEN DAVID R; SIDENSTICK JOHN E 权利人:JENSEN DAVID R; SIDENSTICK JOHN E 摘要:The disclosed invention relates to a process for preparing 5-β-keto-1,2,4-oxadiazoles of formula (I), and conversion of 5-β-keto-1,2,4-oxadiazoles (I) into N-pyrazolyl amidoximes of the formula (II) through reaction with hydrazine. The process is defined by two steps. An amidoxime, which may be prepared in situ, is condensed with a β-keto ester to form a 5-β-keto-1,2,4-oxadiazole. The 5-β-keto-1,2,4-oxadiazole is subsequently reacted with hydrazine to furnish the desired N-pyrazolyl amidoxime. The disclosed invention provides several advantages over the current state of the art for the synthesis of N-pyrazolyl amidoximes, which require the condensation of a pyrzolylamine with an actived substrate and subsequent reaction with hydroxyl amine. N-pyrazolyl amidoximes are useful synthetic intermediates, especially for the preparation of photographic developing chemicals.
专利号:US-6482950-B1 优先权日:1991-05-06 标 题 :Squarylium compounds, and processes and intermediates for the synthesis of these compounds 发明人:GARCIA PAULINA P; LEE JOHN W; MARSHALL JOHN L; MCGOWAN DONALD A; PUTTICK ANTHONY J; SPENCER THOMAS K; STROUD STEPHEN G; TELFER STEPHEN J; ZURAW MICHAEL J 权利人:POLAROID CORP 摘要:Squarylium compounds of the formula: n wherein Q 1 and Q 2 are each independently a pyrylium, thiopyrylium, selenopyrylium, benzpyrylium, benzthiopyrylium or benzselenopyrylium nucleus, and R 1 and R 2 are each independently an aliphatic or cycloaliphatic group, can be prepared by reacting a squaric acid derivative of the formula: n with a compound of the formula Q 2 CH 2 R 2 in the presence of a base. The derivatives of Formula II may be prepared by condensing a 2,3,4,4-tetrahalocyclobut-2-en-1-one with a compound of the formula Q 1 CH 2 R 1 in the presence of a base to produce a compound of the formula: n wherein Q 1 and R 1 are as defined above, and X represents chlorine or bromine, and hydrolyzing the compound of Formula III. Alternatively, the derivatives of Formula II may be prepared by reacting a diester, monoacid chloride monoester or diacid chloride of squaric acid with a compound of the formula Q 1 CH 2 R 1 in the presence of a base, followed by hydrolysis of the resultant monoacid chloride or monoester derivative of the compound of Formula II to the parent compound.
专利号:US-2018273464-A1 优先权日:2018-05-25 标题 :Synthesis and in vitro activity of d-lactic acid oligomers 发明人:GOLDBERG JOEL STEVEN; GOODEN DAVID MARTIN 权利人:GOLDBERG JOEL STEVEN; GOODEN DAVID MARTIN 摘要:This invention describes the synthesis and pharmacologic activity of n=2, n=3, n=4, n=5, and n=6 D-lactic acid oligomers. D-lactic acid dimer has pharmacologic activity and sequesters L-lactate, and the other D-lactic acid oligomers have no activity in vitro, but may have pharmacologic activity in vivo as prodrugs of D-lactic acid dimer.
专利号:EP-2013190-A2 优先权日:2006-04-20 标题 :SYNTHESIS OF 5-ß-KETO-1,2,4-OXADIAZOLES AND CONVERSION OF 5-ß-KETO-1,2,4-OXADIAZOLES TO N-PYRAZOLYL AMIDOXIMES
专利号:WO-2007124024-A2 优先权日:2006-04-20 标 题:SYNTHESIS OF 5-ß-KETO-1,2,4-OXADIAZOLES AND CONVERSION OF 5-ß-KETO-1,2,4-OXADIAZOLES TO N-PYRAZOLYL AMIDOXIMES
专利号:US-5919950-A 优先权日:1991-05-06 标 题 :Squarylium compounds, and processes and intermediates for the synthesis of these compounds