专利号:US-6504041-B2 优先权日:1996-11-15 标题 :Synthesis of ruthenium or osmium metathesis catalysts 发明人:GRUBBS ROBERT H; BELDERRAIN TOMAS R; BROWN SETH N; WILHELM THOMAS E 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention relates to the synthesis of highly active ruthenium and osmium carbene metathesis catalyst in good yield from readily available starting materials. The catalysts that may be synthesized are of the general formula n wherein: n M is ruthenium or osmium; n X and X 1 are independently any anionic ligand; n L and L 1 are any neutral electron donor ligand; and, n R and R 1 are each hydrogen or one of the following substituent groups: C 2 -C 20 alkenyl, C 2 -C 20 alkynyl, C 1 -C 20 alkyl, aryl, C 1 -C 20 carboxylate, C 1 -C 20 alkoxy, C 2 -C 20 alkenyloxy, C 2 -C 20 alkynyloxy, aryloxy, C 2 -C 20 alkoxycarbonyl, C 1 -C 20 alkylthio, C 1 -C 20 alkylsulfonyl and C 1 -C 20 alkylsulfinyl. Optionally, the substituent group may be substituted with one or more groups selected from C 1 -C 5 alkyl, halogen, C 1 -C 5 alkoxy, and aryl. When the substitute aryl group is phenyl, it may be further substituted with one or more groups selected from a halogen, a C 1 -C 5 alkyl, or a C 1 -C 5 alkoxy. Specific synthetic protocols for vinyl alkylidene catalysts wherein R is hydrogen and R 1 is —CHCR 12 R 13 and non-vinyl alkylidene catalysts are also disclosed. In addition to the ease of synthesis (typically a one-step synthesis), the reactions generally may be run at or above room temperature and the resulting products usually may be used without extensive post synthesis purification.
专利号:US-6479685-B2 优先权日:1998-01-09 标题 :Metallocene catalysts for synthesis of high-melting polyolefin copolymer elastomers 发明人:WAYMOUTH ROBERT M; KRAVCHENKO RAISA L; MACIEJEWSKI PETOFF JENNIFER; HUNG JOYCE 权利人:TRUSTEES OF THE LELAND STANDAR 摘要:Metallocene catalysts having plural coordination geometries for synthesis of high melting polyolefin copolymers suitable as thermoplastic elastomers. The inventive catalysts comprise unbridged, substituted or unsubstituted cyclopentadienyl metallocene catalysts that are capable of inter-converting between states with different polymerization or copolymerization characteristics, which interconversion is controlled by selecting the substituents of the cyclopentadienyl ligands so that the rate of interconversion of the two states is within several orders of magnitude of the rate of formation of a single polymer chain. Where r i >r f the polymer can be characterized as multiblock; where r i 专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
专利号:WO-2025053792-A1 优先权日:2023-09-06 标题:Collective synthesis of phantomolin family through total synthesis of the sesquiterpene lactone molephantin 发明人:CHIBA SHUNSUKE; PATOURET REMI HENRI LOUIS; LI HOI YEUNG; LAI SOAK KUAN 权利人:UNIV NANYANG TECH 摘要:Disclosed herein are processes to generate an intermediate in the total synthesis of (+)- molephantin or a derivative thereof, and a total synthesis of (+)-molephantin or a derivative thereof. Also disclosed herein are methods of forming a compound of formula XIV and of forming a compound of formula XV, wherein compound of formula XIV and compound of formula XV are as defined in the description.
专利号:WO-2012047907-A9 优先权日:2010-10-04 标题 :Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto 发明人:MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 权利人:HARVARD COLLEGE; MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for a wide variety of substituents at position 5 of the tetracycline ring system.
专利号:US-2017327504-A1 优先权日:2014-10-30 标 题:Synthesis of Substituted 1H-Pyrazolo[3,4-D]Pyrimidines 发明人:ROSE CHRISTOPHER; SILBERGER HERBERT; SCHREINER ERWIN; FELZMANN WOLFGANG; MARAS NENAD 权利人:SANDOZ AG 摘要:The present invention refers to the synthesis and intermediates of substituted bicyclic compounds by using a central 1H-pyrazolo[3,4-d]pyrimidine of formula (I), which is assembled starting from 4,6-dichloropyrimidine carboxylic acid. The invention in particular refers to the synthesis of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one(ibrutinib) and its synthesis intermediates.
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