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    • 8. 发明申请
    • METHOD FOR PRODUCING (-)CIS-3-HYDROXY-1-METHYL-4-(2,4,6-TRIMETHOXYPHENYL)-PIPERIDINE
    • 用于制备( - )顺-3-羟基-1-甲基-4-(2,4,6-三甲氧基苯基) - 哌啶
    • WO99037615A1
    • 1999-07-29
    • PCT/EP1998/008327
    • 1998-12-18
    • C07D211/42C07D211/72C07D211/74C07D405/04
    • C07D405/04C07D211/42C07D211/72C07D211/74
    • Disclosed is a method for producing (-)cis-3-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-piperidine characterised in that 1-methyl-piperidine-4-one is converted into hydrobromide, subsequently transformed with bromine into 3(R,S)-bromine-1-methyl-4-oxo-piperidine-hydrobromide and reacted with 1,3,5-trimethoxybenzol to form 3(R,S)-bromine-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine-hydrobromide. By stirring the reaction solution into an organic solvent, 3(R,S)-bromine-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine-hydrobromide is initially isolated as a solid and subsequently the product is mixed with water and converted into 3(R,S)-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine by means of stirring. The product thus prepared is catalytically hydrogenated into a racemic 3,4-cis-alcahol and subsequently, enantiomerically pure (-)cis-3-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-piperidine is obtained by separation of racemic mixtures with chiral auxiliary reagents from racemic 3,4-cis alcohol.
    • 它是用于制备方法( - )顺-3-羟基-1-甲基-4-(2,4,6-三甲氧基苯基) - 哌啶描述,其特征在于1-甲基哌啶-4- 上转化成氢溴酸盐,然后用溴,得到3(R,S) - 溴-1-甲基-4-氧代 - 哌啶氢溴酸盐,并进一步与1,3,5-三甲氧基苯向3(R,S) - 溴 1-甲基-4-(2,4,6-三甲氧基苯基)-1,2,3,6-四氢 - 吡啶氢溴酸盐反应。 通过在有机溶剂中最初3(R,S)搅拌反应溶液溴-1-甲基-4-(2,4,6-三甲氧基苯基)-1,2,3,6-四氢 - 吡啶氢溴酸盐,其为固体 分离,并随后加入到与水的产物,并通过搅拌,3(R,S) - 羟基-1-甲基-4-(2,4,6-三甲氧基苯基)-1,2,3,6-四氢 - 吡啶进行反应。 当时工作式产物催化氢化,得到外消旋3,4-顺醇,然后通过与手性辅助试剂外消旋体拆分由外消旋3,4-顺醇的对映体纯的( - )顺-3-羟基-1-甲基-4- (2,4,6-三甲氧基苯基)哌啶获得。
    • 9. 发明申请
    • OXIME DERIVATIVES, HYDRAZONE DERIVATIVES, AND USE THEREOF
    • OXIME衍生物,HYDRAZONE衍生物及其用途
    • WO1998016499A1
    • 1998-04-23
    • PCT/JP1997003585
    • 1997-10-07
    • SHIONOGI & CO., LTD.MASUI, MoriyasuTANIMOTO, NorihikoNISHIDA, Kuniyoshi
    • SHIONOGI & CO., LTD.
    • C07C251/36
    • C07D213/30A01N37/50A01N41/06A01N41/10A01N43/40A01N43/46A01N43/80A01N47/16C07C251/36C07C251/48C07C251/52C07C251/54C07C251/74C07C259/06C07D207/12C07D211/42C07D211/46C07D211/58C07D211/72C07D243/08C07D261/02C07D295/185C07D295/26C07D333/16C07D401/12
    • Compounds having bactericidal activities and represented by general formula (I) and salts and hydrates thereof wherein R represents an optionally substituted aryl, an optionally substituted alkyl or the like; R represents an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted aryl, an optionally substituted heterocyclic group or the like; R represents an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted arylsulfonyl, an optionally substituted heterocyclic group or the like; R and R , which may be the same or different, represent each a hydrogen atom, an optionally substituted alkyl, or an optionally substituted alkoxy, or R and R may form together with the adjacent nitrogen atom an optionally substituted monocycle or polycycle; X and Y, which may be the same or different, represents each an oxygen atom or NR (wherein R represents a hydrogen atom, an optionally substituted alkyl, an optionally substituted aryl, an optionally substituted alkanoyl, or an optionally substituted aroyl); Z represents an oxygen atom or a sulfur atom; and a wavy line ( SIMILAR ) represents the configuration of an E isomer, a Z isomer, or a mixture thereof.
    • 具有杀菌活性并由通式(I)表示的化合物及其盐和水合物,其中R 1表示任选取代的芳基,任选取代的烷基等; R 2表示任选取代的烷基,任选取代的烯基,任选取代的炔基,任选取代的芳基,任选取代的杂环基等; R 3表示任选取代的烷基,任选取代的烯基,任选取代的炔基,任选取代的芳基磺酰基,任选取代的杂环基等; R 4和R 5可以相同或不同,表示氢原子,任选取代的烷基或任选取代的烷氧基,或者R 4和R 5可以与 相邻氮原子,任选取代的单环或多环; X和Y可以相同或不同,表示每个氧原子或NR 6(其中R 6表示氢原子,任选取代的烷基,任选取代的芳基,任选取代的烷酰基或 任选取代的芳酰基); Z表示氧原子或硫原子; 和波浪线(SIMILAR)表示E异构体,Z异构体或其混合物的构型。