专利号:US-10308588-B2 优先权日:2014-12-15 标 题 :Synthesis of amides and amines from aldehydes or ketones by heterogeneous metal catalysis 发明人:CÓRDOVA ARMANDO; PALO-NIETO CARLOS; AFEWERKI SAMSON 权利人:ORGANOFUEL SWEDEN AB 摘要:A mild and efficient synthesis of primary amines and amides from aldehydes or ketones using a heterogeneous metal catalyst and amine donor is disclosed. The initial heterogeneous metal-catalyzed reaction between the carbonyl and the amine donor components is followed by the addition of a suitable acylating agent component in one-pot, thus providing a catalytic one-pot three-component synthesis of amides. Integration of enzyme catalysis allows for eco-friendly one-pot co-catalytic synthesis of amides from aldehyde and ketone substrates, respectively. The process can be applied to asymmetric synthesis or to the co-catalytic one-pot three-component synthesis of capsaicin and its analogues from vanillin or vanillyl alcohol. A co-catalytic reductive amination/dynamic kinetic resolution (dkr) relay sequence for the asymmetric synthesis of optically active amides from ketones is disclosed. Implementation of a catalytic reductive amination/kinetic resolution (kr) relay sequence produces the corresponding optically active amide product and optical active primary amine product with the opposite stereochemistry from the starting ketones.
专利号:US-11168050-B2 优先权日:2014-03-27 标 题 :Efficient synthesis of amines and amides from alcohols and aldehydes by using cascade catalysis 发明人:CÓRDOVA ARMANDO; BERGLUND PER; ANDERSON MATTIAS; AFEWERKI SAMSON 权利人:XP CHEMISTRIES AB 摘要:The present invention relates generally to an eco-friendly methodology for the conversion of alcohols and aldehydes to amines and amides using an integrated enzyme cascade system with metal- and organocatalysis. More specifically, the present invention relates to synthesis of capsaicinoids starting from vanillin alcohol and using a combination of an enzyme cascade system and catalysts. Furthermore, the method also relates to synthesis of capsaicinoids derivatives starting from vanillin alcohol derivatives and using a combination of an enzyme cascade system and catalysts.
专利号:US-2024229089-A1 优先权日:2021-04-30 标 题 :A process for enzymatic synthesis of amides from amines and carboxylic acids or esters 发明人:LIN SHUANGZHENG; CORDOVA ARMANDO; DEIANA LUCA; IBRAHEM ISMAIL 权利人:XP CHEMISTRIES AB 摘要:The present invention relates to A process for enzymatic synthesis of amides of formula (III) from amines of formula (I) and compounds of formula (II). characterized in that the lipase is immobilized on a rotary bed reactor or on a spin-fixed-bed reactor and a Dean-Stark apparatus is used for dehydration.
专利号:US-12188057-B2 优先权日:2017-10-20 标 题 :Primer-independent DNA polymerases and their use for DNA synthesis 发明人:SALAS FALGUERAS MARGARITA; REDREJO RODRIGUEZ MODESTO; KRUPOVIC MART; FORTERRE PATRICK 权利人:CONSEJO SUPERIOR INVESTIGACION; PASTEUR INSTITUT 摘要:The present invention provides an isolated peptide of SEQ ID NO: 1 needed for primase active as well as new replicative DNA polymerase enzymes, preferably that of SEQ ID NO: 2, comprising said peptide. Thus, these DNA polymerases are endowed with priming activity and do not require externally provided primers for initiating and performing DNA amplification. These polymerases are able to carry out a faithful and processive de novo DNA synthesis of DNA templates in the absence of pre-synthetized primers. Therefore, these enzymes of the invention act both as primases and DNA polymerases. Furthermore, they show translesion synthesis capacity, so that they may be useful not only for whole-genome amplification but also for the amplification of damaged DNAs. The invention further refers to methods for amplifying templates DNAs using these enzymes.
专利号:US-5094782-A 优先权日:1990-12-24 标 题:Synthesis of capsacin derivatives and their use as an analgesic drug and vessel dilation drug 发明人:CHEN ING-JUN; YEH JWU-LAI 权利人:NAT SCIENCE COUNCIL REPUBLIC CHINA 摘要:Nonanoyl vanillylamide succinate was synthesized from synthetic capsaicin (nonanoyl vanillylamide) and succinic anhydride. The antinociceptive and cardiovascular effects of nonanoyl vanillylamide and its derivatives were investigated. We found that nonanoyl vanillylamide and nonanoyl vanillylamide succinate strongly inhibited the writhing response, led to the vascular smooth muscle relaxation, produces bradycardia and a fall of blood pressure. The potency of nonanoyl vanillylamide succinate was found to be slight greater than that of nonanoyl vanillylamide, when compared with the same molar dose/kg of their administrations.
专利号:US-12325864-B2 优先权日:2021-05-06 标题:Recombinant virus vector (RVV) for inhibiting epidermal growth factor receptor (EGFR) activity and method of making an agent/target cell complex to increase cetuximab-like protein (CLP) production 发明人:THOMPSON BRADLEY G 权利人:KINASE PHARMA INC 摘要:The present disclosure relates to one or more agents, therapies, treatments, and methods of use of the agents and/or therapies and/or treatments for increasing production of a Cetuximab-like protein (CLP) by a subject that is administered the agent, therapy or treatment. Embodiments of the present disclosure can be used as a therapy or a treatment for a subject that has a condition that may benefit from reducing the DNA synthesis of genes that regulate cellular growth and proliferation.
1: Walker J, Ley JP, Schwerzler J, Lieder B, Beltran L, Ziemba PM, Hatt H, Hans J, Widder S, Krammer GE, Somoza V. Nonivamide, a capsaicin analogue, exhibits anti-inflammatory properties in peripheral blood mononuclear cells and U-937 macrophages. Mol Nutr Food Res. 2017 Feb;61(2). doi: 10.1002/mnfr.201600474. Epub 2016 Nov 15. doi: 10.1080/00498254.2017.1344790. Epub 2017 Jul 6. doi: 10.1002/jcla.22142. Epub 2017 Jan 19. doi: 10.1039/c4fo00435c. Epub 2014 Nov 25. doi: 10.1007/s00421-016-3357-3. Epub 2016 Mar 22. doi: 10.2147/JPR.S118329. eCollection 2016. 8: Hochkogler CM, Lieder B, Rust P, Berry D, Meier SM, Pignitter M, Riva A, Leitinger A, Bruk A, Wagner S, Hans J, Widder S, Ley JP, Krammer GE, Somoza V. A 12-week intervention with nonivamide, a TRPV1 agonist, prevents a dietary-induced body fat gain and increases peripheral serotonin in moderately overweight subjects. Mol Nutr Food Res. 2017 May;61(5). doi: 10.1002/mnfr.201600731. Epub 2017 Feb 22. doi: 10.1139/cjpp-2013-0158. Epub 2013 Oct 21. doi: 10.3109/10837450.2015.1135346. Epub 2016 Jan 11. doi: 10.1002/mnfr.201200846. Epub 2013 Aug 9. doi: 10.1002/jcb.25052. 13: Heck R, Lukić MŽ, Savić SD, Daniels R, Lunter DJ. Ex vivo skin permeation and penetration of nonivamide from and in vivo skin tolerability of film-forming formulations containing porous silica. Eur J Pharm Sci. 2017 Aug 30;106:34-40. doi: 10.1016/j.ejps.2017.05.045. Epub 2017 May 22. doi: 10.1002/ejp.719. Epub 2015 Apr 30.
合成参考文献
摘要:S13 | EUCOSMETICS | Combined Inventory of Ingredients Employed in Cosmetic Products (2000) and Revised Inventory (2006) | DOI:10.5281/zenodo.2624118 摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664