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-7825244-B2 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
专利号:US-5204456-A 优先权日:1986-04-08 标题:Derivatives of nucleosides and their use for the synthesis of oligonucleotides 发明人:MOLKO DIDIER; SCHULHOF JEAN-CLAUDE; TEOULE ROBERT 权利人:COMMISSARIAT ENERGIE ATOMIQUE 摘要:The invention relates to derivatives of nucleosides and their use for the synthesis of oligonucleotides. These derivatives are in accordance with the formula: (I) in which B represents a radical derived from guanine, cytosine or adenine, whose exocylic NH group is protected by the group with R1 representing a hydrogen atom or a alkyl radical and R2 a hydrogen atom, and alkyl radical, an alkoxy radical and optionally substituted aryloxy radical, R3 represents a hydrogen atom, the dimethoxytrityl radical or the radical R4 represents a hydrogen atom, the radical of formula: or a radical suitable for the synthesis of polynucelotides and R5 represents a hydrogen atom or the protected or unprotected hydroxyl OH radical.
专利号:US-9688644-B2 优先权日:2009-04-30 标 题 :Synthesis of Tetracyclines and intermediates thereto 发明人:MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M 权利人:HARVARD COLLEGE 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 substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
专利号:US-2005014954-A1 优先权日:2001-11-22 标 题:Pyrrole synthesis 发明人:OHRLEIN REINHOLD; BAISCH GABRIELE 摘要:The invention relates to a novel process for the preparation of N-substituted pyrroles, especially of formula (V), wherein the radicals are as defined in the description, by intermolecular aza-Wittig reaction starting from organic azides and 1,4-dioxo compounds. The invention relates also to novel iminophosphorane intermediates for this synthesis. The resulting pyrroles are useful, for example, in the organic synthesis of pharmaceuticals or other active substances and chemicals.
专利号:US-8026383-B2 优先权日:2001-07-06 标题:Process for the preparation of intermediates useful in the synthesis of statin derivatives 发明人:OEHRLEIN REINHOLD; BAISCH GABRIELE; END NICOLE; BURKHARDT STEPHAN; STUDER MARTIN 权利人:BASF SE 摘要:The invention relates to novel synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I n nwherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or —N(CH 3 )OCH 3 , R a is a hydroxy-protecting group and R b is a carboxy-protecting group, and, as well as to the compound of formula I, to further new intermediates and methods for their preparation by Friedel-Crafts acylation.
摘要:Yoshimatsu, M., Science of Synthesis Knowledge Updates, (2016) 2, 396. 参考文献:10.1038/srep42096 摘要:Liu CH, Chen XY, Qin PW, Qi ZQ, Ji MS, Liu XY, Babu PV, Li XH, Cui ZN. Synthesis, Fungicidal Activity, and Structure Activity Relationship of β-Acylaminocycloalkylsulfonamides against Botrytis cinerea. Sci Rep. 2017 Feb 08;7():42096.