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1.发明授权PROCESS FOR PRODUCING N-tert-BUTYL-2-PYRAZINECARBOXAMIDE AND N-tert-BUTYL-2-PIPERAZINECARBOXAMIDE 失效用于生产的N-叔丁基-2-吡嗪羧基酰胺和N-叔丁基-2-哌嗪
公开(公告)号：EP0680955B1
公开(公告)日：2002-09-18
申请号：EP95900932.5
申请日：1994-11-21
发明人： WATANABE, Nanao Koei Chemical Co., Ltd. , ASAHI, Sadao Koei Chemical Co., Ltd. , KURANISHI, Hideki Koei Chemical Co., Ltd. , KURAHASHI, Takashi Koei Chemical Co., Ltd.
IPC分类号： C07D241/04 , C07D241/24
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.
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2.发明授权PROCESS FOR PRODUCING OPTICALLY ACTIVE N-TERT-BUTYL- 2-PIPERAZINE- CARBOXAMIDE 失效用于生产光学活性的N-叔丁基-2- PIPERAZINCARBOXAMIDAMID
公开(公告)号：EP0705824B1
公开(公告)日：2002-08-07
申请号：EP95916018.5
申请日：1995-04-20
发明人： WATANABE, Nanao Koei Chemical Co., Ltd. , TOKUDA, Yoko Koei Chemical Co., Ltd. , KIKEGAWA, Kenichi Koei Chemical Co., Ltd. , KURANISHI, Hideki Koei Chemical Co., Ltd. , KURAHASHI, Takashi 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.
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3.发明公开PROCESS FOR PRODUCING OPTICALLY ACTIVE N-TERT-BUTYL-2-PIPERAZINECARBOXAMIDE AND METHOD OF RACEMIZING THE AMIDE 失效用于生产光学活性的N-叔丁基过氧化-2- PIPERAZINECARBOXAMID AND METHOD FOR酰胺的外消旋化
公开(公告)号：EP0705824A1
公开(公告)日：1996-04-10
申请号：EP95916018.5
申请日：1995-04-20
发明人： WATANABE, Nanao Koei Chemical Co., Ltd. , TOKUDA, Yoko Koei Chemical Co., Ltd. , KIKEGAWA, Kenichi Koei Chemical Co., Ltd. , KURANISHI, Hideki Koei Chemical Co., Ltd. , KURAHASHI, Takashi 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： 一种制备光学活性的N-叔丁基-2-哌嗪羧基酰胺有用的方法，例如，在药物中间体在由（R，S）-N-叔丁基-2- piperazinecarboxyamide的光学分辨率的高光学纯度 与使用光学活性的乳酸，苹果酸或酒石酸的。 残留在上述光学拆分步骤无用的对映体对映体可以有效地通过在碱性化合物的存在外消旋化的光学活性的N-叔丁基-2-哌嗪羧基酰胺和 - 影响再次光学拆分中使用。
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4.发明公开PROCESS FOR PRODUCING N-tert-BUTYL-2-PYRAZINECARBOXAMIDE AND N-tert-BUTYL-2-PIPERAZINECARBOXAMIDE 失效用于生产的N-叔丁基-2-吡嗪羧基酰胺和N-叔丁基-2-哌嗪。
公开(公告)号：EP0680955A1
公开(公告)日：1995-11-08
申请号：EP95900932.5
申请日：1994-11-21
发明人： WATANABE, Nanao Koei Chemical Co., Ltd. , ASAHI, Sadao Koei Chemical Co., Ltd. , KURANISHI, Hideki Koei Chemical Co., Ltd. , KURAHASHI, Takashi Koei Chemical Co., Ltd.
IPC分类号： C07D241/04 , C07D241/24
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.
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