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1. 发明申请

WO1994019328A1 PYRAZINE DERIVATIVE 审中-公开
标题翻译：吡嗪衍生物
公开(公告)号：WO1994019328A1
公开(公告)日：1994-09-01
申请号：PCT/JP1994000254
申请日：1994-02-18
申请人： KOEI CHEMICAL CO., LTD. , TOIDA, Ichiro , YAMAMOTO, Setsuko , WATANABE, Nanao , URA, Toshikazu
发明人： KOEI CHEMICAL CO., LTD.
IPC分类号： C07D241/24
CPC分类号： C07D241/24
摘要： A pyrazine derivative represented by general formula (1) and excellent in the effect of curing infectious diseases caused by various acid-fast bacteria, wherein R1 represents octyl or pivaloyloxymethyl.
摘要翻译：由通式（1）表示的吡嗪衍生物，由各种耐酸细菌引起的感染性疾病的治疗效果优异，其中R1表示辛基或新戊酰氧基甲基。

2. 发明申请

WO1998015531A1 PROCESS FOR PREPARING ACID SALTS OF 'gamma'-(PIPERIDYL)BUTYRIC ACID 审中-公开
标题翻译：制备γ-（哌啶）丁酸的酸盐的方法
公开(公告)号：WO1998015531A1
公开(公告)日：1998-04-16
申请号：PCT/JP1997003594
申请日：1997-10-07
申请人： KOEI CHEMICAL CO., LTD. , SAKAI, Toshito , NAGAOKA, Masayo , KANNO, Ken
发明人： KOEI CHEMICAL CO., LTD.
IPC分类号： C07D211/34
CPC分类号： C07D211/34 , C07D213/55
摘要： A process for preparing acid salts (2) of gamma -(piperidyl)butyric acid by hydrogenating an acid salt (1) of gamma -(pyridyl)butyric acid (preferably, one prepared through the following steps (a) and (b) and having a content of acid salts (3) of bis(pyridylethyl)acetic acid of not more than 3 % by weight) in a solvent in the presence of a catalyst, wherein a rhodium, palladium or ruthenium catalyst is used as the catalyst. Step (a): a vinylpyridine compound (4) is reacted with a diester (5) of malonic acid in the presence of a base to prepare a diester (6) of 2-(pyridylethyl)malonic acid. Step (b): the diester (6) prepared in the step (a) is hydrolyzed and decarboxylated in an aqueous acid solution to prepare the acid salt (1) of gamma -(pyridyl)butyric acid.
摘要翻译：通过氢化γ-（吡啶基）丁酸的酸性盐（1）（优选通过以下步骤（a）和（b）制备的酸）的盐酸盐（1），制备γ-（哌啶基）丁酸的酸式盐（2）在催化剂存在下，在溶剂中含有不超过3重量％的双（吡啶基乙基）乙酸的酸式盐（3）的含量，其中使用铑，钯或钌催化剂作为催化剂。步骤（a）：将乙烯基吡啶化合物（4）与丙二酸二酯（5）在碱的存在下反应，制备2-（吡啶基乙基）丙二酸二酯（6）。步骤（b）：将步骤（a）中制备的二酯（6）在酸性水溶液中水解脱羧，制备γ-（吡啶基）丁酸的酸式盐（1）。

3. 发明申请

WO1995014675A1 PROCESS FOR PRODUCING N-tert-BUTYL-2-PYRAZINECARBOXAMIDE AND N-tert-BUTYL-2-PIPERAZINECARBOXAMIDE 审中-公开
标题翻译：生产N-叔丁基-2-吡嗪酰胺和N-叔丁基-2-哌啶甲酰胺的方法
公开(公告)号：WO1995014675A1
公开(公告)日：1995-06-01
申请号：PCT/JP1994001972
申请日：1994-11-21
申请人： KOEI CHEMICAL CO., LTD. , WATANABE, Nanao , ASAHI, Sadao , KURANISHI, Hideki , KURAHASHI, Takashi
发明人： KOEI CHEMICAL CO., LTD.
IPC分类号： C07D241/04
CPC分类号： C07D241/24 , C07D241/04
摘要： A process for producing an N-tert-butyl-2-pyrazinecarboxamide represented by general formula (2) by the reaction of a cyanopyrazine represented by general formula (1) with tert-butyl alcohol in the presence of sulfuric acid; and a process for producing an N-tert-butyl-2-piperazinecarboxamide represented by general formula (3) by the hydrogenation of an N-tert-butyl-2-pyrazinecarboxamide represented by the above general formula (2) in the presence of Raney nickel or Raney cobalt.
摘要翻译：由通式（1）表示的氰基吡嗪与叔丁醇在硫酸存在下反应制备由通式（2）表示的N-叔丁基-2-吡嗪甲酰胺的方法; 和由通式（3）表示的N-叔丁基-2-哌嗪甲酰胺通过在阮内存在下氢化上述通式（2）表示的N-叔丁基-2-吡嗪甲酰胺的方法，镍或阮内钴。

4. 发明申请

WO1998003483A1 PROCESS FOR THE PREPARATION OF PIPERIDINES 审中-公开
标题翻译：制备哌啶的方法
公开(公告)号：WO1998003483A1
公开(公告)日：1998-01-29
申请号：PCT/JP1997002495
申请日：1997-07-18
申请人： KOEI CHEMICAL CO., LTD.
发明人： KOEI CHEMICAL CO., LTD. , HARADA, Katsutoshi
IPC分类号： C07D211/02
CPC分类号： C07D295/023 , C07D211/02
摘要： A process for the preparation of piperidines by catalytic reduction of pyridines, whereby the catalytic reduction of a pyridine can be completed even with a relatively small amount of a catalyst and the formation of by-products having boiling points near that of an objective piperidine can be inhibited to attain the preparation of the piperidine in a high yield, characterized by charging a pyridine and at least 2 % by weight (based on the pyridine) of a stabilized nickel catalyst into a pressure reactor and conducting the catalytic reduction of the pyridine under agitation at a reaction temperature of 140 to 250 DEG C under a hydrogen pressure kept at 30 to 100 kgf/cm (2.9 x 10 to 9.8 x 10 Pa) by introducing hydrogen into the reactor.
摘要翻译：通过吡啶的催化还原制备哌啶的方法，即使使用相对少量的催化剂也可以完成吡啶的催化还原，并且形成沸点接近目标哌啶的副产物可以是抑制以高产率制备哌啶，其特征在于将吡啶和至少2重量％（基于吡啶）的稳定的镍催化剂装入压力反应器中并在搅拌下进行催化还原吡啶在140〜250℃的反应温度下，通过将氢气引入反应器中，在氢气压力保持在30〜100kgf / cm 2（2.9×10 6〜9.8×10 6 Pa）的条件下进行。

5. 发明申请

WO1995029170A1 PROCESS FOR PRODUCING OPTICALLY ACTIVE N-TERT-BUTYL-2-PIPERAZINECARBOXAMIDE AND METHOD OF RACEMIZING THE AMIDE 审中-公开
标题翻译：用于生产光学活性N-叔丁基-2-哌啶甲酰胺的方法和使酰胺化的方法
公开(公告)号：WO1995029170A1
公开(公告)日：1995-11-02
申请号：PCT/JP1995000777
申请日：1995-04-20
申请人： KOEI CHEMICAL CO., LTD. , WATANABE, Nanao , TOKUDA, Yoko , KIKEGAWA, Kenichi , KURANISHI, Hideki , KURAHASHI, Takashi
发明人： KOEI CHEMICAL CO., LTD.
IPC分类号： C07D241/04
CPC分类号： C07D241/04
摘要： A process for producing optically active N-tert-butyl-2-piperazinecarboxamide useful as, for example, an intermediate for medicines at a high optical purity by the optical resolution of (R,S)-N-tert-butyl-2-piperazinecarboxyamide with the use of optically active lactic, malic or tartaric acid. The antipode remaining as a useless antipode in the above optical resolution step can be used effectively by racemizing optically active N-tert-butyl-2-piperazinecarboxamide in the presence of a basic compound and effecting optical resolution again.
摘要翻译：通过（R，S）-N-叔丁基-2-哌嗪甲酰胺的光学拆分制备用作例如高光学纯度的药物的中间体的光学活性N-叔丁基-2-哌嗪甲酰胺的方法使用光学活性乳酸，苹果酸或酒石酸。在上述光学拆分步骤中作为无用的对映体保留的对映体可以通过在碱性化合物的存在下外消光旋光N-叔丁基-2-哌嗪甲酰胺并再次进行光学拆分而有效地使用。

6. 发明申请

WO1992013840A1 PROCESS FOR PRODUCING 'alpha'-CHLORINATED AMINOMETHYL-PYRIDINES 审中-公开
标题翻译：生产α-氯代氨基甲基吡啶的方法
公开(公告)号：WO1992013840A1
公开(公告)日：1992-08-20
申请号：PCT/JP1992000094
申请日：1992-01-31
申请人： KOEI CHEMICAL CO., LTD. , NABATA, Toshinari
发明人： KOEI CHEMICAL CO., LTD.
IPC分类号： C07D213/61
CPC分类号： C07D213/61
摘要： A process for producing alpha -chlorinated aminomethylpyridines such as 6-chloro-3-aminomethylpyridine by the catalytic reduction of alpha -chlorinated cyanopyridines such as 6-chloro-3-cyanopyridine in the presence of a tertiary amine in a nonaqueous reaction system. alpha -chlorinated aminomethylpyridines can be produced in good yields, because the elimination of the alpha -chlorine atom is inhibited in this process.
摘要翻译：通过在非水反应体系中的叔胺存在下，通过催化还原α-氯代氰基吡啶如6-氯-3-氰基吡啶来生产α-氯代氨基甲基吡啶如6-氯-3-氨基甲基吡啶的方法。 α-氯代氨基甲基吡啶可以以良好的产率生产，因为在该方法中α-氯原子的消除被抑制。

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