专利号:US-4026911-A 优先权日:1976-02-23 标 题:Process for the preparation of ketoalkynoic acids and use of the process in an improved synthesis of 2-(substituted)-cyclo-pentane-1,3,4-triones 发明人:REVERMAN LAWRENCE FRANCIS 权利人:MILES LAB 摘要:Reaction of a 2-methyl-2-(alkenyl)-1,3-dioxolane with an α,ω-dihalogenoalkane to obtain a 2-methyl-2-(ω-chloroalkynyl)-dioxolane, conversion of the latter to a corresponding nitrile, and hydrolysis of the nitrile to form a ketoalkynoic acid is a novel process for preparing the acid. n Use of the process in the synthesis of 2-(substituted)-cyclopentane-1,3,4-triones improves that synthesis.
专利号:US-2009264648-A1 优先权日:2008-01-14 标题:Synthesis of pyrazoles 发明人:CHEW WARREN; WANG ZHENG; CHEAL GLORIA; BERTRAND MARTIAL; POTOSKI JOHN; MIRMEHRABI MAHMOUD; NENCINI ARIANNA; ZANALETTI RICCARDO 权利人:WYETH CORP; SIENA BIOTECH SPA 摘要:The present invention provides compounds and compositions, methods of making them, and methods of using them to modulate α7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.
专利号:WO-2009091832-A1 优先权日:2008-01-14 标题 :Synthesis of pyrazoles
专利号:WO-9506037-A1 优先权日:1993-08-27 标题 :New imidazole derivatives having agonistic or antagonistic activity on the histamine h3 receptor 发明人:VOLLINGA ROELANT CHRISTIAAN; MENGE WIRO MICHAEL PETRUS BERN; TIMMERMAN HENDRIK 权利人:VRIJE UNIVERSITEIT; VOLLINGA ROELANT CHRISTIAAN; MENGE WIRO MICHAEL PETRUS BERN; TIMMERMAN HENDRIK 摘要:The invention relates to new imidazole derivatives of formula (I) having agonistic and antagonistic activity on the histamine H3-receptor. More in particular the invention concerns 4- and 5-substituted aminoalkyl imidazoles and their derivatives. The invention further relates to the synthesis of these compounds, pharmaceutical compositions comprising the said compounds or pharmacological salts thereof, and the use of the compounds as agents having biological activity on the histamine H3-receptor or for the preparation of a pharmaceutical composition.
专利号:US-5268501-A 优先权日:1990-02-08 标 题 :Process for preparing haloketo acid derivatives 发明人:IKEDA TAKAHARU; KAI SEIICHI; MINAI MASAYOSHI 权利人:SUMITOMO CHEMICAL CO 摘要:Process for preparing haloketo acid derivatives [I]: ##STR1## wherein R is H or C 1-6 alkyl, and X is chlorine or bromine, which comprises reacting β-oxo-acid ester [II]: ##STR2## wherein R 1 is H or C 1-6 alkyl, R 2 is C 1-5 alkyl or OR 3 (R 3 is C 1-6 alkyl), and X is the same as above, with nitrosating agent [IV]: n n ONOR.sup.4 [IV] n n wherein R 4 is H, alkyl, halogen or SO 3 H to give 7-halo-2-hydroxyminoheptanoic acid ester [III]: ##STR3## wherein R 1 and X are the same as above, following by reacting the product with aldehyde or ketone; and intermediates therefor, and process for preparing said intermediates. Said haloketo acid derivatives are useful as intermediate for synthesis of cilastatin, which is useful as medicament, especially as dehydropeptidase inhibitor.
专利号:DE-2707128-A1 优先权日:1976-02-23 标 题:PROCESS FOR THE PREPARATION OF KETOALKYNIC ACIDS AND APPLICATION OF THE PROCESS TO AN IMPROVED SYNTHESIS OF 2- (SUBSTITUTE) -CYCLOPENTANE-1,3,4-TRIONEN