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公开(公告)号：US20240150269A1
公开(公告)日：2024-05-09
申请号：US18372980
申请日：2023-09-26
申请人： McMaster University
发明人： Jakob Magolan , Nicholas Jentsch , Xiong Zhang , Mathew Piotrowski , Patrick Darveau , Meghan Fragis , Jarrod Johnson , Nicole Ritchie , Arnav Kaul
IPC分类号： C07C37/14 , B01J21/04 , C07C41/26 , C07C201/12 , C07C253/30 , C07D209/08 , C07D307/80 , C07D311/30 , C07D311/32 , C07J1/00 , C07J7/00
CPC分类号： C07C37/14 , B01J21/04 , C07C41/26 , C07C201/12 , C07C253/30 , C07D209/08 , C07D307/80 , C07D311/30 , C07D311/32 , C07J1/0059 , C07J7/0005
摘要： The present application describes process for preparing an ortho-allylated hydroxy aryl compounds such as compounds of Formula (1) by reacting an allylic alcohol with a hydroxy aryl compound in the presence of aluminum compound selected from alumina and aluminum alkoxides and in a non-protic solvent wherein at least one carbon atom ortho to the hydroxy group in the hydroxy aryl compound is unsubstituted. The present application also includes compounds of Formula (1).
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公开(公告)号：US11795127B2
公开(公告)日：2023-10-24
申请号：US17964347
申请日：2022-10-12
申请人： McMaster University
发明人： Jakob Magolan , Nicholas Jentsch , Xiong Zhang , Mathew Piotrowski , Patrick Darveau , Meghan Fragis , Jarrod Johnson , Nicole Ritchie , Arnav Kaul
IPC分类号： C07C37/14 , C07J7/00 , B01J21/04 , C07D209/08 , C07C41/26 , C07D307/80 , C07C201/12 , C07J1/00 , C07D311/30 , C07D311/32 , C07C253/30
CPC分类号： C07C37/14 , B01J21/04 , C07C41/26 , C07C201/12 , C07C253/30 , C07D209/08 , C07D307/80 , C07D311/30 , C07D311/32 , C07J1/0059 , C07J7/0005
摘要： The present application describes process for preparing an ortho-allylated hydroxy aryl compounds such as compounds of Formula (I) by reacting an allylic alcohol with a hydroxy aryl compound in the presence of aluminum compound selected from alumina and aluminum alkoxides and in a non-protic solvent wherein at least one carbon atom ortho to the hydroxy group in the hydroxy aryl compound is unsubstituted. The present application also includes compounds of Formula (I).
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公开(公告)号：US20180311262A1
公开(公告)日：2018-11-01
申请号：US16020641
申请日：2018-06-27
发明人： Gabriel Martinez Botella , Boyd L. Harrison , Albert Jean Robichaud , Francesco G. Salituro , Richard Thomas Beresis
CPC分类号： A61K31/58 , A61K9/0019 , A61K31/573 , C07J1/0059 , C07J1/007 , C07J1/0074 , C07J3/00 , C07J5/0015 , C07J5/0053 , C07J7/00 , C07J7/002 , C07J7/007 , C07J7/0085 , C07J13/007 , C07J15/00 , C07J21/00 , C07J31/006 , C07J43/003
摘要： Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein , R1, R2, R3a, R3b, R4a, R4b, R5, R6, and R7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
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公开(公告)号：US20180265540A1
公开(公告)日：2018-09-20
申请号：US15982284
申请日：2018-05-17
CPC分类号： C07J1/007 , C07J1/0059 , C07J1/0066 , C07J21/00
摘要： A process is provided for the making of estetrol starting from a 3-A-oxy-estra-1,3,5(10),15-tetraen-17-one, wherein A is an C1-C5 alkyl group, preferably a methyl group, or a C7-C12 benzylic group, preferably a benzyl group. This process is particularly suitable to industry.
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公开(公告)号：US09353145B2
公开(公告)日：2016-05-31
申请号：US14350456
申请日：2012-10-09
申请人： ZACH SYSTEM
发明人： Yvon Derrien , Patricia Poirier , Massimiliano Forcato , Tony Pintus , Livius Cotarca , Sebastien Meunier , Laurence Graindorge
CPC分类号： C07J43/003 , C07J1/0059 , C07J31/003 , C07J31/006
摘要： The present invention relates to a process for the preparation of 17-substituted steroids and, more particularly, to an improved method of synthesizing abiraterone or derivatives thereof in high yield and purity by means of a key 3-formate intermediate.
摘要翻译： 本发明涉及一种制备17-取代的类固醇的方法，更具体地说，涉及通过关键的3-甲酸中间体以高产率和纯度合成阿非特酮或其衍生物的改进方法。
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公开(公告)号：US20150344518A1
公开(公告)日：2015-12-03
申请号：US14649702
申请日：2013-12-10
发明人： Robert N. Hanson , Kinh-Luan Dao
IPC分类号： C07J41/00
CPC分类号： C07J41/0072 , C07B2200/05 , C07J1/0059 , C07J21/006 , C07J41/00 , C07J43/003 , C07J71/0015
摘要： Compounds useful for molecular imaging of cells expressing estrogen receptors are provided. Also provided are intermediates for making the compounds and methods of making the compounds using a modular convergent strategy. Further, methods of making the intermediates are described, as well as methods of diagnosing disease in a subject by using the compounds as imaging agents.
摘要翻译： 提供了可用于表达雌激素受体的细胞分子成像的化合物。 还提供了用于制备化合物的中间体和使用模块化收敛策略制备化合物的方法。 此外，描述了制备中间体的方法，以及通过使用化合物作为成像剂来诊断受试者的疾病的方法。
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公开(公告)号：US20150336926A1
公开(公告)日：2015-11-26
申请号：US14758906
申请日：2013-12-23
发明人： John HARTWIG , Patrick FIER
IPC分类号： C07D333/76 , C07C41/22 , C07C231/12 , C07C67/307 , C07B39/00 , C07C269/06 , C07C253/30 , C07D209/08 , C07J1/00 , C07D209/88 , C07C17/361 , C07C45/63
CPC分类号： C07D333/76 , C07B39/00 , C07C17/361 , C07C41/22 , C07C45/63 , C07C67/307 , C07C231/12 , C07C253/30 , C07C269/06 , C07D209/08 , C07D209/88 , C07D213/89 , C07J1/00 , C07J1/0059 , C07C25/13 , C07C25/18 , C07C25/22 , C07C69/76 , C07C49/807 , C07C43/225 , C07C233/65 , C07C233/15 , C07C255/50
摘要： The invention provides compositions and methods of using the compositions in fluorinating aryl precursors containing a leaving group replaceable by a fluorine atom. The compositions include a metal ion source, a electrophilic fluorine source, a base, and a compound, which is an aryl precursor of the aryl fluoride, and which has a leaving group replaceable by the fluorine atom. Exemplary methods of the invention make use of such compositions and methods to prepare an aryl fluoride compound. In an exemplary embodiment, the electrophilic fluorine source is a source of 18F.
摘要翻译： 本发明提供使用该组合物的氟化芳族前体的组合物和方法，其含有可被氟原子替代的离去基团。 组合物包括金属离子源，亲电氟源，碱和作为芳基氟化物的芳基前体的化合物，并且具有可被氟原子替代的离去基团。 本发明的示例性方法利用这种组合物和方法制备芳基氟化合物。 在一个示例性实施方案中，亲电氟源是18F的来源。
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公开(公告)号：US09150516B2
公开(公告)日：2015-10-06
申请号：US13444676
申请日：2012-04-11
申请人： Tobias Ritter , Pingping Tang
发明人： Tobias Ritter , Pingping Tang
IPC分类号： C07D233/10 , C07D233/28 , C07C67/307 , C07C41/22 , C07C201/12 , C07B39/00 , C07C209/74 , C07C45/63 , C07C17/16 , C07J1/00
CPC分类号： C07D233/28 , C07B39/00 , C07B2200/05 , C07C17/16 , C07C41/22 , C07C45/63 , C07C67/307 , C07C201/12 , C07C209/74 , C07D233/10 , C07J1/0059 , C07C205/12 , C07C211/52 , C07C25/13 , C07C25/18 , C07C43/225 , C07C69/734 , C07C49/697 , C07C69/76
摘要： Methods for fluorinating organic compounds are described herein.
摘要翻译： 本文描述了氟化有机化合物的方法。
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公开(公告)号：US20130331585A1
公开(公告)日：2013-12-12
申请号：US13912000
申请日：2013-06-06
发明人： Matthew Duncton , Michael D. Burke
IPC分类号： C07F5/02 , C07J1/00 , C07C17/263
CPC分类号： C07F5/025 , C07C17/263 , C07C2601/02 , C07J1/0059 , C07J31/006 , Y02P20/55 , C07C22/08
摘要： Provided are protected cyclopropylboronic acids that include a substituted cyclopropyl group and a boronic ester group having a protecting group. The protecting group is a pinene-derived iminodiacetic acid (PIDA) group or PIDA-based group.
摘要翻译： 提供包括取代的环丙基和具有保护基的硼酸酯基的保护的环丙基硼酸。 保护基是蒎烯衍生的亚氨基二乙酸（PIDA）组或基于PIDA的组。
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10.发明申请公开(公告)号：US20130137885A1
公开(公告)日：2013-05-30
申请号：US13578062
申请日：2011-02-08
IPC分类号： C07J1/00
CPC分类号： C07J1/00 , C07J1/0059
摘要： The invention relates to a process for the preparation of a compound of formula wherein R1 and R2 are as defined in the description, by reaction of a compound of formula (II) with a base.Compound (I) is an intermediate useful in the preparation of gestodene.
摘要翻译： 本发明涉及制备下式化合物的方法，其中R 1和R 2如说明书中所定义，通式（Ⅱ）化合物与碱反应。 化合物（I）是可用于制备孕二烯酮的中间体。
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