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1. 发明申请

WO1996009300A1 NOVEL INTERMEDIATE FOR PRODUCTION AND PROCESS FOR PRODUCING PYRIDINE DERIVATIVE 审中-公开
标题翻译：用于生产吡啶衍生物的生产和方法的新的中间体
公开(公告)号：WO1996009300A1
公开(公告)日：1996-03-28
申请号：PCT/JP1995001911
申请日：1995-09-21
申请人： TAIHO PHARMACEUTICAL CO., LTD. , UNIVESITY OF FLORIDA , WATANABE, Syotaro , KEM, William, R. , LEE, Hun, Ju , KAJITANI, Makoto , MARUHASHI, Kazuo
发明人： TAIHO PHARMACEUTICAL CO., LTD. , UNIVESITY OF FLORIDA
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D213/50 , C07D401/06
摘要： The invention relates to: (1) a compound represented by formula (V), a tautomer thereof, and a mixture of both; (2) a process for producing compound (V), tautomer thereof, or mixture thereof as mentioned in item (1) by the reaction of N-vinylpiperidone represented by formula (I) with a nicotinic ester represented by general formula (II) (R being lower alkyl) in the presence of a sodium alkoxide; (3) a process for producing the pyridine derivative represented by formula (III) by producing compound (V), tautomer thereof, or mixture thereof according to the process described in item (2) and treating the product with an acid; and (4) a process for producing the pyridine derivative represented by formula (IV) by further treating the acid-treated compound described in item (3) with a base. The pyridine derivatives (III) and (IV) can thus be produced in an industrial manner safely, economically, readily and efficiently without using dangerous reagents.
摘要翻译：本发明涉及：（1）由式（V）表示的化合物，其互变异构体和两者的混合物; （2）通过式（I）表示的N-乙烯基哌啶酮与由通式（II）表示的烟酸酯反应（1）所示的（1）所述的化合物（V），互变异构体或其混合物的方法 R是低级烷基）在醇盐存在下反应; （3）根据第（2）项所述的方法，通过制备化合物（V），其互变异构体或其混合物，并用酸处理该产物，制备由式（III）表示的吡啶衍生物的方法; 和（4）通过用碱进一步处理式（3）所述的酸处理化合物来制备由式（Ⅳ）表示的吡啶衍生物的方法。因此，吡啶衍生物（III）和（IV）可以安全，经济，容易和有效地以工业方式生产，而不使用危险的试剂。

2. 发明申请

WO1995011879A1 PROCESS FOR PRODUCING ACID-ADDITION SALT OF Z-ISOMER OF TRIPHENYLETHYLENE COMPOUND 审中-公开
标题翻译：生产三苯乙烯化合物的Z-异构体酸的添加剂的方法
公开(公告)号：WO1995011879A1
公开(公告)日：1995-05-04
申请号：PCT/JP1994001782
申请日：1994-10-25
申请人： TAIHO PHARMACEUTICAL CO., LTD. , SHINOZAKI, Fumihiko , NAGASAWA, Hiroshi , MARUHASHI, Kazuo
发明人： TAIHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C217/18
CPC分类号： C07C217/18 , C07C213/08
摘要： A process for producing an acid-addition salt of a Z-isomer of a compound represented by general formula (I) (wherein R and R represent each lower alkyl, or are combined together with the nitrogen atom to which they are bonded to thereby form a nitrogenous heterocyclic group which may bear other heteroatom(s); R and R represent each hydrogen, lower alkyl, hydroxy, lower alkoxy, lower alkylcarbonyloxy, arylcarbonyloxy wherein the benzene ring may be substituted by one or two groups selected from among lower alkyl, lower alkoxy, halogen and cyano, benzylcarbonyloxy, mono- or di(lower alkyl)aminocarbonyloxy, or mono- or di(aryl)aminocarbonyloxy; R represents lower alkyl or halogen; and n represents 1 to 6), which process comprises heating an E-isomer of a compound represented by general formula (I) or an acid-addition salt thereof, either alone or as a mixture thereof with a Z-isomer of a comound represented by general formula (I) or an acid-addition salt thereof, in an organic solvent containing hydrobromic acid.
摘要翻译：一种制备通式（I）表示的化合物的Z-异构体的酸加成盐的方法（其中R 1和R 2代表每个低级烷基，或与氮原子相结合它们被键合从而形成可含有其它杂原子的含氮杂环基; R 3和R 4代表各自的氢，低级烷基，羟基，低级烷氧基，低级烷基羰基氧基，芳基羰基氧基，其中苯环可以是被一个或两个选自低级烷基，低级烷氧基，卤素和氰基的基团取代，苄基羰基氧基，一或二（低级烷基）氨基羰基氧基或一或二（芳基）氨基羰基氧基; R 5表示低级烷基或卤素 ; n表示1至6），该方法包括将通式（I）表示的化合物的E-异构体或其酸加成盐单独或作为其与组合的Z-异构体的混合物由通式（I）表示的化合物或其酸加成盐含有氢溴酸的厌氧溶剂。

3. 发明授权

US5565611A Process for preparing acid addition salt of Z-isomer of triphenylethylene compound 失效
标题翻译：制备三苯乙烯化合物Z-异构体的酸加成盐的方法
公开(公告)号：US5565611A
公开(公告)日：1996-10-15
申请号：US446736
申请日：1995-06-06
申请人： Shinozaki Fumihiko , Nagasawa Hiroshi , Maruhashi Kazuo
发明人： Shinozaki Fumihiko , Nagasawa Hiroshi , Maruhashi Kazuo
IPC分类号： C07C213/08 , C07C217/18 , C07C213/10
CPC分类号： C07C217/18 , C07C213/08
摘要： The present invention provides a process for preparing an acid addition salt of the Z-isomer of a compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 represent a lower alkyl group, or taken together with the nitrogen atom to which they are attached, form a nitrogen-containing heterocyclic group optionally containing other hetero atom or atoms; R.sup.3 and R.sup.4 represent H, a lower alkyl group, OH, a lower alkoxy group, a lower alkylcarbonyloxy group, an arylcarbonyloxy group optionally substituted with 1-2 substituents selected from lower alkyl, lower alkoxy, halo and CN on the benzene ring, a benzylcarbonyloxy group, a mono- or di(lower alkyl)aminocarbonyloxy group or a mono- or di(aryl)aminocarbonyloxy group; R.sup.5 represents a lower alkyl group or halo; and n represents 1-6, characterized in that the E-isomer of the compound of the formula (I) or its acid addition salt, singly or in admixture with the Z-isomer or its acid addition salt, is heated in an organic solvent containing hydrobromic acid.
摘要翻译：本发明提供了制备式（I）化合物的Z-异构体的酸加成盐的方法，其中R 1和R 2表示低级烷基，或与它们所在的氮原子一起形成任选含有其它杂原子或原子的含氮杂环基; R3和R4表示H，低级烷基，OH，低级烷氧基，低级烷基羰氧基，任选被选自苯环上的选自低级烷基，低级烷氧基，卤素和CN的1-2个取代基取代的芳羰基氧基，一或二（低级烷基）氨基羰基氧基或一或二（芳基）氨基羰基氧基; R5表示低级烷基或卤素; 并且n表示1-6，其特征在于式（I）化合物的E-异构体或其酸加成盐单独或与Z-异构体或其酸加成盐混合，在有机溶剂中加热含氢溴酸。

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