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-6683189-B1 优先权日:1996-02-26 标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support 发明人:DERVAN PETER B; BAIRD ELDON 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.
专利号:US-9446995-B2 优先权日:2012-05-21 标 题:Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions 发明人:CHONG HYUN-SOON 权利人:CHONG HYUN-SOON; ILLINOIS INST OF TECH 摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
专利号:US-10189803-B2 优先权日:2008-02-22 标题 :Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions 发明人:CHONG HYUN-SOON 权利人:CHONG HYUN SOON; ILLINOIS INSTITUTE OF TECH 摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
专利号:US-11926589-B2 优先权日:2019-07-09 标 题 :Process for the synthesis of non-racemic cyclohexenes 发明人:REISMAN SARAH; ROMBOLA MICHAEL; LADD CAROLYN L; MCLAUGHLIN MARTIN JOHN; ZUEND STEPHAN; GOETZ ROLAND 权利人:BASF CORP; CALIFORNIA INST OF TECHN 摘要:This invention relates to a process for the synthesis of a non-racemic cyclohexene compound of formula (I) by a Diels-Alder reaction of a compound of formula (II) with a compound of formula (III) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and Y have the meanings as defined in the description in the presence of a catalyst comprising at least one m-valent metal cation M m+ wherein the metal M is selected from Scandium (Sc), Yttrium (Y), Lanthanum (La), Cerium (Ce), Praseodymium (Pr), Neodymium (Nd), Promethium (Pm), Samarium (Sm), Europium (Eu), Gadolinium 15 (Gd), Terbium (Tb), Dysprosium (Dy), Holmium (Ho), Erbium (Er), Thulium (Tm), Ytterbium (Yb), Lutetium (Lu), Gallium (Ga) and Indium (In), and m is an integer of 1, 2 or 3, and a chiral ligand of the formula (IV) wherein R 10a , R 10b , R 10c , R 10d , R 10a′ , R 10b′ , R 10c′ , R 10d′ , Z and Z′ have the meanings as defined in the description.
专利号:WO-2021014395-A1 优先权日:2019-07-24 标题:Process for the synthesis of deuterated capsaicin, capsaicinoids and synthetic capsaicin analogs 发明人:ORUGANTI SRINIVAS; AMRUTAPU SRAVANTH KUMAR; SAMPATH MAGESH; SEN SAIKAT 权利人:DR REDDY’S INST OF LIFE SCIENCES 摘要:The present application provides novel processes for the synthesis of deuterated intermediates of capsaicinoids, particularly II, III, IV and V of capsaicinoids, relating to pharmaceutical applications. The invention also provides novel intermediates of compounds of formula IX, XIV, XV, XVI, XVII, XVIII, XX and XXI utilized in the process of making deuterated capsaicin II, III, IV and V.
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