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1. 发明公开

US20240294449A1 PROCESS FOR THE SYNTHESIS OF PROPARGYLIC ALCOHOL BY REACTING FORMALDEHYDE WITH ACETYLENE IN THE PRESENCE OF A HOMOGENEOUS COPPER CATALYST 审中-公开
公开(公告)号：US20240294449A1
公开(公告)日：2024-09-05
申请号：US18571761
申请日：2022-06-10
申请人： BASF SE
发明人： Thomas SCHAUB , Grigory Andre SHEVCHENKO , A. Stephen K. HASHMI , Nikolai Amadeus SITTE
IPC分类号： C07C29/42
CPC分类号： C07C29/42
摘要： A process to produce propargylic alcohol, wherein acetylene is reacted with formaldehyde in the liquid phase in the presence of a copper catalyst and at least one phosphine.

2. 发明申请

US20170305827A1 METHOD FOR PRODUCING SPECIFIC ALPHA, BETA-UNSATURATED ALDEHYDES 审中-公开
公开(公告)号：US20170305827A1
公开(公告)日：2017-10-26
申请号：US15518355
申请日：2015-10-15
申请人： DSM IP ASSETS B.V.
发明人： Werner BONRATH , Thomas NETSCHER , Jan SCHUETZ , Bettina WUESTENBERG
IPC分类号： C07C45/51 , C07C11/12 , C07C47/225 , C07C5/23 , C07C2601/16
CPC分类号： C07C45/512 , C07C5/23 , C07C11/12 , C07C29/42 , C07C47/225 , C07C2523/46 , C07C2527/14 , C07C2601/16 , C07C33/14
摘要： The present invention relates to an improved method for producing specific α, β-unsaturated aldehydes.

3. 发明申请

US20170057937A1 Process for the preparation of Efavirenz and devices suitable therefore 有权
标题翻译：因此制备依法韦仑和装置的方法
公开(公告)号：US20170057937A1
公开(公告)日：2017-03-02
申请号：US14837500
申请日：2015-08-27
申请人： MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFTEN E.V.
发明人： Camille A. Correia , Kerry Gilmore , David Tyler McQuade , Peter H. Seeberger
IPC分类号： C07D265/18 , B01J19/00 , C07C33/50 , C07C29/00 , C07C29/68 , C07C45/00 , C07C265/12 , C07F1/08
CPC分类号： 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
摘要： 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.
摘要翻译：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。

4. 发明申请

US20160347778A1 ALKENES AS ALKYNE EQUIVALENTS IN RADICAL CASCADES TERMINATED BY FRAGMENTATIONS 有权
标题翻译： ALKYES作为ALKYNE等价物在分段放出的放射性CASCAD
公开(公告)号：US20160347778A1
公开(公告)日：2016-12-01
申请号：US15143669
申请日：2016-05-02
申请人： The Florida State University Research Foundation, Inc.
发明人： Igor V. Alabugin , Sayantan Mondal , Rana K. Mohamed
IPC分类号： C07F7/22 , C07C17/093 , C07C37/055 , C07D239/26 , C07C45/00 , C07D333/08 , C07D213/16 , C07C1/32 , C07C253/00
CPC分类号： C07F7/2208 , C07C1/325 , C07C17/093 , C07C29/42 , C07C41/01 , C07C41/16 , C07C41/30 , C07C45/00 , C07C45/67 , C07C67/333 , C07C253/30 , C07C2603/10 , C07C2603/24 , C07D213/16 , C07D239/26 , C07D333/08 , C07C255/50 , C07C33/28 , C07C43/1787 , C07C43/166 , C07C43/225 , C07C43/20 , C07C69/618 , C07C15/24 , C07C15/28 , C07C49/784
摘要： Disclosed are methods for rerouting radical cascade cyclizations by using alkenes as alkyne equivalents. The reaction sequence is initiated by a novel 1,2 stannyl shift which achieves chemo- and regioselectivity in the process. The radical “hopping” leads to the formation of the radical center necessary for the sequence of selective cyclizations and fragmentations to follow. In the last step of the cascade, the elimination of a rationally designed radical leaving group via β-C—C bond scission aromatizes the product without the need for external oxidant. The Bu3Sn moiety, which is installed during the reaction sequence, allows further functionalization of the product via facile reactions with electrophiles as well as Stille and Suzuki cross-coupling reactions. This selective radical transformation opens a new approach for the controlled transformation of enynes into extended polycyclic structures of tunable dimensions.
摘要翻译：公开了通过使用烯烃作为炔等价物来重新路由自由基级联环化的方法。反应顺序由一个新的1,2-甲锡烷基转移引发，在该过程中实现了化学和区域选择性。激进的“跳跃”导致了选择性环化和碎裂序列所必需的激进中心的形成。在级联的最后一步中，通过β-C-C键断裂消除合理设计的自由基离去基团使产物芳构化而不需要外部氧化剂。在反应顺序期间安装的Bu 3 Sn部分允许通过与亲电试剂以及Stille和Suzuki交叉偶联反应的容易反应进一步官能化产物。这种选择性的根本性转化开辟了一种新颖的方法，可以控制烯炔转变为可调节尺寸的延伸多环结构。

5. 发明申请

US20160107977A1 METHODS OF SYNTHESIS OF INGENOL AND INTERMEDIATES THEREOF 审中-公开
标题翻译：其合成方法及其中间体
公开(公告)号：US20160107977A1
公开(公告)日：2016-04-21
申请号：US14894406
申请日：2014-05-28
申请人： LEO LABORATORIES LIMITED
发明人： Phillipe S. BARAN , Lars JØRGENSEN , Christian A. KUTTRUFF , Steven J. MCKERRALL , Chien-Hung YEH
IPC分类号： C07C67/08 , C07C45/68
CPC分类号： C07C67/08 , C07C17/02 , C07C29/00 , C07C29/42 , C07C35/28 , C07C45/30 , C07C45/40 , C07C45/64 , C07C45/65 , C07C45/68 , C07C45/72 , C07C49/743 , C07C2602/20 , C07C2603/40 , C07D317/70 , C07F7/1804 , C07C23/28 , C07C49/693 , C07C49/627 , C07C49/727 , C07C47/21
摘要： The present invention relates generally to methods of synthesis of diterpene heterocylic compounds. More particularly, the present invention relates to efficient methods of synthesis of ingenol (Formula (21), CAS 30220-46-3), from a compound of formula (1). The present invention also provides for various advantageous intermediates along the synthetic route of ingenol. Efficient synthesis of ingenol is important in the design and synthesis of related analogues, such as ingenol-3-angelate.
摘要翻译：本发明一般涉及双萜杂环化合物的合成方法。更具体地说，本发明涉及由式（1）化合物合成烯内酯（式（21），CAS 30220-46-3））的有效方法。本发明还提供了沿着联合烯醇的合成途径的各种有利的中间体。在有关类似物的设计和合成中，如烯雌醇-3-天竺葵素，有效合成烯醇是非常重要的。

6. 发明申请

US20140275639A1 Novel Ethynylation Catalyst And Method Of Making Same 有权
标题翻译：新型乙炔化催化剂及其制备方法
公开(公告)号：US20140275639A1
公开(公告)日：2014-09-18
申请号：US14203664
申请日：2014-03-11
申请人： BASF Corporation
发明人： Rostam Madon , Peter Nagel , Scott Hedrick , Deepak Thakur
IPC分类号： B01J23/72 , B01J23/843 , C07C29/42
CPC分类号： B01J23/8437 , B01J21/10 , B01J23/72 , B01J35/0006 , B01J35/008 , B01J35/023 , B01J35/026 , B01J37/035 , B01J37/06 , B01J37/08 , B01J2523/00 , C07C29/42 , C07C33/046 , B01J2523/12 , B01J2523/17 , B01J2523/22 , B01J2523/31 , B01J2523/41 , B01J2523/54
摘要： A novel catalyst useful in the ethynylation of formaldehyde to butynediol is formed by precipitating copper and bismuth from a salt solution of such metals, utilizing an alkali metal hydroxide as the precipitating agent to deposit copper and bismuth hydroxide as a coating around a siliceous carrier particle.
摘要翻译：通过使用碱金属氢氧化物作为沉淀剂沉淀铜和铋从这种金属的盐溶液沉淀，形成用于甲醛与丁炔二炔的乙炔化反应的新催化剂，以沉积铜和氢氧化铋作为二氧化硅载体颗粒周围的涂层。

7. 发明申请

US20120029237A1 Autocatalytic Process for the Synthesis of Chiral Propargylic Alcohols 失效
标题翻译：用于合成手性炔丙醇的自动催化方法
公开(公告)号：US20120029237A1
公开(公告)日：2012-02-02
申请号：US12740617
申请日：2010-04-09
申请人： Nicka Chinkov , Aleksander Warm , Erick Carreira
发明人： Nicka Chinkov , Aleksander Warm , Erick Carreira
IPC分类号： C07C29/44 , C07C231/12 , C07C213/00
CPC分类号： C07C231/18 , C07B2200/07 , C07C29/42 , C07C213/00 , C07C2601/02 , C07C33/28 , C07C215/70 , C07C233/25
摘要： An autocatalytic process for the synthesis of chiral propargylic alcohols.
摘要翻译：用于合成手性炔丙醇的自催化方法。

8. 发明申请

US20120022283A1 METHODS FOR MAKING VALERENIC ACID DERIVATIVES AND THEIR USE 有权
标题翻译：制备戊酸衍生物及其用途的方法
公开(公告)号：US20120022283A1
公开(公告)日：2012-01-26
申请号：US13138227
申请日：2010-01-22
申请人： Johann Mulzer , Jürgen Ramharter , Steffen Hering , Sophia Khom
发明人： Johann Mulzer , Jürgen Ramharter , Steffen Hering , Sophia Khom
IPC分类号： C07C57/26 , C07C69/732
CPC分类号： C07C69/608 , A61K31/16 , C07C29/42 , C07C57/26 , C07C69/732 , C07C231/02 , C07C233/02 , C07C233/10 , C07C233/16 , C07C243/32 , C07C2602/24 , C07D307/93
摘要： The present invention is directed to compounds, intermediates and methods for making valerenic acid and its derivatives as well as the use of such compounds as GABAA receptor ligands.
摘要翻译：本发明涉及制备戊酰酸及其衍生物的化合物，中间体和方法以及这些化合物如GABA A受体配体的用途。

9. 发明申请

US20110295042A1 METHOD FOR PREPARING PROPARGYLIC ALCOHOL CATALYZED BY 2-MORPHOLINOISOBORNANE-10-THIOL 有权
标题翻译：用于制备由2-吗啉代氧杂环己烷-10-THIOL催化的丙烷醇的方法
公开(公告)号：US20110295042A1
公开(公告)日：2011-12-01
申请号：US12787961
申请日：2010-05-26
申请人： Biing-Jiun UANG , Ping-Yu Wu , Hsyueh-Liang Wu
发明人： Biing-Jiun UANG , Ping-Yu Wu , Hsyueh-Liang Wu
IPC分类号： C07C41/18 , C07C29/36
CPC分类号： C07C29/42 , C07B2200/07 , C07C41/30 , C07C33/28 , C07C33/483 , C07C43/23
摘要： A method for preparing a propargylic alcohol catalyzed by 2-morpholinoisobornane-10-thiol (MITH) is disclosed, which includes reacting R1CHO with R2CCH in the presence of R3ZnR4 and MITH, wherein each of R1, R2, R3, and R4, independently, is optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkylsilyl, heterocycloalkyl, heterocycloalkenyl, aryl, aryloxy, or heteroaryl. The method can give enantioenriched propargylic alcohols with good enantioselective at low loading of MITH.
摘要翻译：公开了一种制备由2-吗啉代异丁硼烷-10-硫醇（MITH）催化的炔丙醇的方法，该方法包括在R3ZnR4和MITH的存在下使R1CHO与R2CCH反应，其中R 1，R 2，R 3和R 4各自独立地为是任选取代的烷基，烯基，环烷基，环烯基，烷基甲硅烷基，杂环烷基，杂环烯基，芳基，芳氧基或杂芳基。该方法可以在MITH的低负载下给出具有良好对映选择性的对映异构醇的炔丙醇。

10. 发明申请

US20110004028A1 PROCESS FOR PRODUCTION OF DIALCOHOL, PROCESS FOR PRODUCTION OF ALLYLHALIDE COMPOUND, AND ALLYLCHLORIDE COMPOUND 审中-公开
标题翻译：生产二醇的方法，生产全氟化合物的方法和全氯化合物
公开(公告)号：US20110004028A1
公开(公告)日：2011-01-06
申请号：US12920669
申请日：2009-03-02
申请人： Toshiya Takahashi
发明人： Toshiya Takahashi
IPC分类号： C07C29/16 , C07C17/354 , C07C21/215
CPC分类号： C07C29/17 , C07C17/16 , C07C21/215 , C07C29/42 , C07C33/02 , C07C33/048
摘要： Disclosed are: an advantageous production process for a carotenoid intermediate; and others. Specifically disclosed are: a process for producing a dialcohol represented by formula (1), which is characterized by reacting a Grignard reagent with an acetylene gas in an organic solvent at a temperature of 30° C. or higher to prepare an ethynyl magnesium halide and subsequently reacting the ethynyl magnesium halide with methacrolein; a process for producing an allylhalide compound represented by formula (3) [wherein X represents a halogen atom: and the wavy line means the compound is either of E/Z geometric isomers or a mixture thereof], which is characterized by reducing a dialcohol represented by formula (1) with hydrogen to produce a triene alcohol represented by formula (2) [wherein the wavy line is as defined above] and halogenating the triene alcohol; and an allylchloride compound represented by formula (4) [wherein the wavy line is as defined above].
摘要翻译：公开了：类胡萝卜素中间体的有利生产方法; 和别的。具体公开的是：制备由式（1）表示的二醇的方法，其特征在于在30℃或更高的温度下使格氏试剂与乙炔气在有机溶剂中反应，制备乙炔基卤化镁和随后使乙炔基卤化镁与甲基丙烯醛反应; 一种由式（3）表示的烯丙基卤化合物的制备方法[其中X表示卤素原子，波浪线表示化合物是E / Z几何异构体或其混合物），其特征在于还原二醇通过式（1）与氢反应以制备由式（2）表示的三烯醇[其中波浪线如上所定义]并卤化三烯醇; 和由式（4）表示的烯丙基氯化物[其中波浪线如上所定义]。

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