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1.发明申请Synthesis of Racemic Amphetamine Derivatives by Cuprate Addition Reaction with Aziridine Phosphoramidate Compounds 有权通过与氮丙啶氨基磷酸酯化合物的铜酸盐加成反应合成外消旋苯丙胺衍生物公开(公告)号：US20150183810A1
公开(公告)日：2015-07-02
申请号：US14327209
申请日：2014-07-09
申请人： Chemapotheca LLC , Harold Meckler , Brian Thomas Gregg , Jie Yang
发明人： Harold Meckler , Brian Thomas Gregg , Jie Yang
IPC分类号： C07F9/22 , C07F9/564 , C07F9/02 , C07C209/62
CPC分类号： C07F9/564 , C07C209/62 , C07F9/2458 , C07F9/2475 , C07C211/27
摘要： The invention includes processes for the synthesis of amphetamine, dexamphetamine, methamphetamine, derivatives of these, including their salts, and novel precursors and intermediates obtained thereby, by synthesizing aziridine phosphoramidate compounds in specified solvents at specified temperatures, and then converting to a novel aryl or aryl-alkyl phosphoramidate precursors using an organometallic compound such as a copper salt, where the novel aryl or aryl-alkyl phosphoramidate precursor is then easily converted to the target compounds using known reactions.
摘要翻译： 本发明包括合成苯丙胺，右旋苯丙胺，甲基苯丙胺，它们的衍生物，包括它们的盐的方法，以及由此获得的新型前体和中间体，通过在指定温度下合成特定溶剂中的氮丙啶氨基磷酸酯化合物，然后转化为新的芳基或 使用有机金属化合物如铜盐的芳基 - 烷基氨基磷酸酯前体，其中新的芳基或芳基 - 烷基氨基磷酸酯前体然后使用已知的反应容易地转化成目标化合物。
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2.发明申请Synthesis of Chiral Amphetamine Derivatives by Stereospecific, Regioselective Cuprate Addition Reaction with Aziridine Phosphoramidate Compounds 有权通过与氮丙啶氨基磷酸酯化合物的立体特异性，区域选择性铜酸盐加成反应合成手性苯酚衍生物公开(公告)号：US20150183716A1
公开(公告)日：2015-07-02
申请号：US14189630
申请日：2014-02-25
申请人： Je Yang , Harold Meckler , Brian Thomas Gregg , Chemapotheca, LLC
发明人： Harold Meckler , Brian Thomas Gregg , Jie Yang
IPC分类号： C07C209/68 , C07F9/564
CPC分类号： C07F9/564 , C07B2200/07 , C07C209/62 , C07F9/2458 , C07F9/2475 , C07C211/27
摘要： The invention includes processes for the synthesis of amphetamine, dexamphetamine, methamphetamine, derivatives of these, including their salts, and novel precursors and intermediates obtained thereby, by synthesizing aziridine phosphoramidate compounds in specified solvents at specified temperatures, and then converting to a novel aryl or aryl-alkyl phosphoramidate precursors using an organometallic compound such as a copper salt, where the novel aryl or aryl-alkyl phosphoramidate precursor is then easily converted to the target compounds using known reactions,
摘要翻译： 本发明包括合成苯丙胺，右旋苯丙胺，甲基苯丙胺，它们的衍生物，包括它们的盐的方法，以及由此获得的新型前体和中间体，通过在指定温度下合成特定溶剂中的氮丙啶氨基磷酸酯化合物，然后转化为新的芳基或 使用有机金属化合物例如铜盐的芳基 - 烷基氨基磷酸酯前体，其中新的芳基或芳基 - 烷基氨基磷酸酯前体然后使用已知的反应容易地转化为目标化合物，
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3.发明授权Process for and intermediates in the preparation of canfosfamide and its salts 有权用于制备卡非司酮及其盐的方法和中间体公开(公告)号：US08334266B2
公开(公告)日：2012-12-18
申请号：US13429065
申请日：2012-03-23
申请人： William A. Boulanger , Steven J. Collier , Stephen A. Eastham , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernandez Abad , R. Jason Herr , Hans J. Kjaersgaard , Harold Meckler , Robert E. Polomski , Steven R. Schow , Pavel E. Zhichkin
发明人： William A. Boulanger , Steven J. Collier , Stephen A. Eastham , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernandez Abad , R. Jason Herr , Hans J. Kjaersgaard , Harold Meckler , Robert E. Polomski , Steven R. Schow , Pavel E. Zhichkin
CPC分类号： C07K5/0205 , A61K38/00 , C07F9/2408 , C07F9/2458 , C07K5/0215 , C07K5/0606 , C07K5/06191
摘要： A process for and intermediates in the preparation of canfosfamide and its salts. Some of the intermediates have anticancer activity.
摘要翻译： 一种在制备头孢噻吩及其盐的过程和中间体。 一些中间体具有抗癌活性。
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4.发明申请公开(公告)号：US20120238772A1
公开(公告)日：2012-09-20
申请号：US13429065
申请日：2012-03-23
申请人： William A. Boulanger , Steven J. Collier , Stephen A. Eastham , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernández Abad , R. Jason Herr , Hans J. Kjaersgaard , Harold Meckler , Robert E. Polomski , Steven R. Schow , Pavel E. Zhichkin
发明人： William A. Boulanger , Steven J. Collier , Stephen A. Eastham , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernández Abad , R. Jason Herr , Hans J. Kjaersgaard , Harold Meckler , Robert E. Polomski , Steven R. Schow , Pavel E. Zhichkin
IPC分类号： C07F9/24 , C07C323/59
CPC分类号： C07K5/0205 , A61K38/00 , C07F9/2408 , C07F9/2458 , C07K5/0215 , C07K5/0606 , C07K5/06191
摘要： A process for and intermediates in the preparation of canfosfamide and its salts. Some of the intermediates have anticancer activity.
摘要翻译： 一种在制备头孢噻吩及其盐的过程和中间体。 一些中间体具有抗癌活性。
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公开(公告)号：US08067605B2
公开(公告)日：2011-11-29
申请号：US12956601
申请日：2010-11-30
IPC分类号： C07D211/22
CPC分类号： C07D211/14 , C07D211/22
摘要： Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III: The processes involve reacting a compound of formula Ia, IIa or IIIa with isobutyrate or an isobutyrate equivalent.
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公开(公告)号：US07498345B2
公开(公告)日：2009-03-03
申请号：US10943276
申请日：2004-09-17
IPC分类号： A61K31/445
CPC分类号： C07D211/14 , C07D211/22
摘要： Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III: The processes involve reacting a compound of formula Ia, IIa or IIIa with isobutyrate or an isobutyrate equivalent.
摘要翻译： 公开了制备式I，II或III的哌啶衍生物化合物的方法：该方法包括使式Ia，IIa或IIIa的化合物与异丁酸酯或异丁酸酯当量反应。
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7.发明申请Process for and intermediates in the preparation of canfosfamide and its salts 失效用于制备卡非司酮及其盐的方法和中间体公开(公告)号：US20060135409A1
公开(公告)日：2006-06-22
申请号：US11018391
申请日：2004-12-21
申请人： William Boulanger , Steven Collier , Stephen Eastham , Dennis Edie , Ronan Guevel , Pedro Abad , R. Herr , Hans Kjaersgaard , Harold Meckler , Robert Polomski , Steven Schow , Pavel Zhichkin
发明人： William Boulanger , Steven Collier , Stephen Eastham , Dennis Edie , Ronan Guevel , Pedro Abad , R. Herr , Hans Kjaersgaard , Harold Meckler , Robert Polomski , Steven Schow , Pavel Zhichkin
CPC分类号： C07K5/0205 , A61K38/00 , C07F9/2408 , C07F9/2458 , C07K5/0215 , C07K5/0606 , C07K5/06191
摘要： A process for and intermediates in the preparation of canfosfamide and its salts. Some of the intermediates have anticancer activity.
摘要翻译： 一种在制备头孢噻吩及其盐的过程和中间体。 一些中间体具有抗癌活性。
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8.发明申请Catalytic hydrogenation of nitriles to produce capsaicinoid derivatives and amine compounds, and methods for purifying and obtaining the polymorphs thereof 审中-公开腈类催化氢化制备辣椒素衍生物和胺化合物，以及纯化和获得其多晶型物的方法公开(公告)号：US20060047171A1
公开(公告)日：2006-03-02
申请号：US10927493
申请日：2004-08-27
申请人： Harold Meckler , Karl Popp , Bingidimi Mobele , Paul Isbester , Bruce Elder , Paul Vogt , Benjamin Littler , Stephen Eastham , David Reed , Luckner Ulysse , Michael Uttley
发明人： Harold Meckler , Karl Popp , Bingidimi Mobele , Paul Isbester , Bruce Elder , Paul Vogt , Benjamin Littler , Stephen Eastham , David Reed , Luckner Ulysse , Michael Uttley
IPC分类号： A61K31/16 , C07C233/24
CPC分类号： C07C235/34 , C07C231/12
摘要： Processes for preparing an amine compound by catalytically hydrogenating a precursor nitrile compound. In a particular aspect, the present hydrogenation process occurs in a dipolar organic solvent in the presence of a palladium/carbon catalyst and a strong anhydrous protic acid. In a further aspect, the preferred embodiment relates to a process for deprotecting a compound to produce an amine compound. In yet a further aspect, the preferred embodiment relates to amine products produced by the present processes. These amine products may be used for a variety of purposes.
摘要翻译： 通过催化氢化前体腈化合物制备胺化合物的方法。 在一个特定方面，本发明的氢化方法在钯/碳催化剂和强无水质子酸的存在下在偶极有机溶剂中进行。 在另一方面，优选的实施方案涉及使化合物脱保护以制备胺化合物的方法。 在另一方面，优选实施方案涉及通过本方法制备的胺产物。 这些胺产物可用于各种目的。
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公开(公告)号：US20230149342A1
公开(公告)日：2023-05-18
申请号：US17522866
申请日：2021-11-09
申请人： KYLE OLSON , HAROLD MECKLER , MARCUS BRACKEEN , MARIO TREMBLAY
发明人： KYLE OLSON , HAROLD MECKLER , MARCUS BRACKEEN , MARIO TREMBLAY
IPC分类号： A61K31/352 , C07C37/74 , C07D311/78 , A61K31/05 , B01J31/14 , B01D3/10 , B01D1/08 , B01D3/14 , B01D11/04 , B01D39/20 , A23L33/105
CPC分类号： A61K31/352 , C07C37/74 , C07D311/78 , A61K31/05 , B01J31/143 , B01D3/10 , B01D1/08 , B01D3/143 , B01D11/0492 , B01D39/2068 , A23L33/105 , A61K2236/55 , B01D2011/002
摘要： The present invention describes a method which outlines a process for conversion of CBD to a Δ9-tetrahydrocannabinol (Δ9-THC) compound or derivative thereof involving treating a naturally produced CBD intermediate compound with an organoaluminum-based Lewis acid catalyst, under conditions effective to produce the Δ9-tetrahydrocannabinol compound or derivative thereof at a relatively high concentration. The source of the CBD is from industrial hemp having less than 0.3% Δ9-THC and extracting and purifying a CBD distillate or isolate or a combination thereof. This procedure will produce Δ9-THC that is essentially free from any other cannabinoids other than some trace amounts of the initial CBD starting material, or about 95% Δ9-THC and 2-4% CBD. Another aspect of the present invention relates to a process for further purification and enrichment of the Δ9-THC using distillation and collecting an essentially pure fraction of Δ9-THC using additional distillation or enrichment form of purification. Included are methods and processes to scale the reaction from the lab to large scale manufacturing. Included are methods for adding a molecule marker to authenticate high purity Δ9-THC products. Formulations and uses for pharmaceuticals, nutraceuticals, food products, and topicals are also provided.
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公开(公告)号：US08198247B2
公开(公告)日：2012-06-12
申请号：US11018391
申请日：2004-12-21
申请人： William A. Boulanger , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernandez Abad , R. Jason Herr , Harold Meckler , Steven R. Schow , Pavel E. Zhichkin
发明人： William A. Boulanger , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernandez Abad , R. Jason Herr , Harold Meckler , Steven R. Schow , Pavel E. Zhichkin
IPC分类号： A61K38/14
CPC分类号： C07K5/0205 , A61K38/00 , C07F9/2408 , C07F9/2458 , C07K5/0215 , C07K5/0606 , C07K5/06191
摘要： A process for and intermediates in the preparation of canfosfamide and its salts. Some of the intermediates have anticancer activity.
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