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公开(公告)号：US20170057937A1
公开(公告)日：2017-03-02
申请号：US14837500
申请日：2015-08-27
Inventor： Camille A. Correia , Kerry Gilmore , David Tyler McQuade , Peter H. Seeberger
IPC: C07D265/18 , B01J19/00 , C07C33/50 , C07C29/00 , C07C29/68 , C07C45/00 , C07C265/12 , C07F1/08
CPC classification number: C07D265/18 , B01J19/0093 , B01J2219/00792 , B01J2219/00795 , B01J2219/0081 , B01J2219/00813 , B01J2219/00833 , B01J2219/00835 , B01J2219/0086 , B01J2219/00867 , B01J2219/00873 , B01J2219/00889 , B01J2219/00894 , B01J2219/00963 , C07C29/00 , C07C29/42 , C07C29/68 , C07C33/50 , C07C45/00 , C07C45/46 , C07C265/12 , C07C2601/02 , C07F1/08 , C07C49/80
Abstract: The invention relates to a process for the preparation of Efavirenz via an efficient transition metal catalyzed cyclization, to a device suitable to perform such process as well as to novel intermediates.
Abstract translation: 本发明涉及通过有效的过渡金属催化环化制备依法韦仑的方法，涉及适用于进行这种方法的装置以及新型中间体。
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公开(公告)号：US09676735B2
公开(公告)日：2017-06-13
申请号：US14837500
申请日：2015-08-27
Inventor： Camille A. Correia , Kerry Gilmore , David Tyler McQuade , Peter H. Seeberger
IPC: C07D265/18 , C07C265/12 , B01J19/00 , C07F1/08 , C07C29/00 , C07C29/68 , C07C45/00 , C07C33/50
CPC classification number: C07D265/18 , B01J19/0093 , B01J2219/00792 , B01J2219/00795 , B01J2219/0081 , B01J2219/00813 , B01J2219/00833 , B01J2219/00835 , B01J2219/0086 , B01J2219/00867 , B01J2219/00873 , B01J2219/00889 , B01J2219/00894 , B01J2219/00963 , C07C29/00 , C07C29/42 , C07C29/68 , C07C33/50 , C07C45/00 , C07C45/46 , C07C265/12 , C07C2601/02 , C07F1/08 , C07C49/80
Abstract: The invention relates to a process for the preparation of Efavirenz via an efficient transition metal catalyzed cyclization, to a device suitable to perform such process as well as to novel intermediates.
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公开(公告)号：US09802952B2
公开(公告)日：2017-10-31
申请号：US14904671
申请日：2014-07-14
Inventor： Daniel Kopetzki , David Tyler McQuade , Peter H. Seeberger , Kerry Gilmore
IPC: C07D493/18 , B01J19/24
CPC classification number: C07D493/18 , B01J19/245 , B01J2219/24
Abstract: The present invention is directed to a method for continuous production of dihydroartemisinin and also artemisinin derivatives derived from dihydroartemisinin by using artemisinin or dihydroartemisinic acid (DHAA) as starting material as well as to a continuous flow reactor for producing dihydroartemisinin as well as the artemisinin derivatives. It was found that the reduction of artemisinin to dihydroartemisinin in a continuous process requires a special kind of reactor and a special combination of reagents comprising a hydride reducing agent, at least one activator such as an inorganic activator, at least one solid base, at least one aprotic solvent and at least one C1-C5 alcohol.
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4.发明申请METHOD AND APPARATUS FOR THE SYNTHESIS OF DIHYDROARTEMISININ AND ARTEMISININ DERIVATIVES 有权合成二氢TEM IN嗪和TEM IS嗪衍生物的方法与装置公开(公告)号：US20160145265A1
公开(公告)日：2016-05-26
申请号：US14904671
申请日：2014-07-14
Inventor： Daniel Kopetzki , David Tyler McQuade , Peter H. Seeberger , Kerry Gilmore
IPC: C07D493/18 , B01J19/24
CPC classification number: C07D493/18 , B01J19/245 , B01J2219/24
Abstract: The present invention is directed to a method for continuous production of dihydroartemisinin and also artemisinin derivatives derived from dihydroartemisinin by using artemisinin or dihydroartemisinic acid (DHAA) as starting material as well as to a continuous flow reactor for producing dihydroartemisinin as well as the artemisinin derivatives. It was found that the reduction of artemisinin to dihydroartemisinin in a continuous process requires a special kind of reactor and a special combination of reagents comprising a hydride reducing agent, at least one activator such as an inorganic activator, at least one solid base, at least one aprotic solvent and at least one C1-C5 alcohol.
Abstract translation: 本发明涉及通过使用青蒿素或二氢青蒿酸（DHAA）作为起始原料以及用于生产二氢青蒿素的连续流动反应器以及青蒿素衍生物，连续制备二氢青蒿素和源自二氢青蒿素的青蒿素衍生物的方法。 发现在连续方法中将青蒿素还原成二氢青蒿素需要特殊类型的反应器，并且包含氢化物还原剂，至少一种活化剂如无机活化剂，至少一种固体碱的试剂的特殊组合至少 一种非质子溶剂和至少一种C1-C5醇。
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