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2-甲基-2-丙基4-乙基-1-哌嗪羧酸酯置于三氟乙酸体系中,化学反应 0.08H,以94%的收率获得产物n-乙基哌嗪
参考文献:新型苯并咪唑衍生物作为抗真菌剂的合成与研究
标题:新型苯并咪唑衍生物作为抗真菌剂的合成与研究
摘要:多种病原性真菌菌株对抗真菌药物的抵抗性的上升和出现导致对新抗真菌药物的需求增加.过去研发了具有不同作用机理的多种杂环支架.本文中,我们报道了18种烷基化的单,双和三苯并咪唑衍生物的合成和抗真菌活性,它们对哺乳动物细胞的毒性以及在酵母细胞中诱导活性氧(ros)的能力.我们的许多双苯并咪唑化合物对所有测试的真菌菌株均表现出中等至出色的抗真菌活性,Mic值为15.6至0.975μg/ Ml.发现我们的双苯并咪唑类的真菌活性谱取决于烷基链长.
DOI:10.1016/j.Bmc.2016.06.010

专利信息

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-11059914-B2
优先权日:2016-12-21
标题:Method for the continuous synthesis of a diene elastomer with lithium amide initiator
发明人：DIRE CHARLOTTE; DESSENDIER MARIE-HÉLÈNE
权利人:MICHELIN & CIE
摘要:A process for the continuous synthesis of a diene elastomer is provided. The synthesis is conducted by means of n reactors r1 to rn, considered to be continuous stirred-tank reactors, which are equipped with an internal stirring system. The reactors are arranged in series, n varying from 2 to 15, preferably from 2 to 9. The reactor r1 is fed by an input solution comprising a solvent, one or more monomer(s), an anionic polymerization initiator chosen from lithium amides and a polar agent. The conversion by weight C1 in the first reactor is less than 70%, and the total conversion by weight Cn at the outlet of the reactor rn is greater than or equal to 70%.

专利号:US-9121110-B2
优先权日:2002-12-19
标 题 :Quasirandom structure and function guided synthesis methods
发明人：GOULIAEV ALEX HAAHR; HOLTMANN ANETTE; PEDERSEN HENRIK; FRANCH THOMAS
权利人:GOULIAEV ALEX HAAHR; HOLTMANN ANETTE; PEDERSEN HENRIK; FRANCH THOMAS; NUEVOLUTION AS
摘要:The present invention is directed to the synthesis of molecules guided by connector polynucleotides (CPNs) capable of hybridizing to complementary connector polynucleotides (CCPNs) harboring at least one functional entity comprising at least one reactive group. At least one of the CCPNs is capable of hybridizing to at least two CPNs. Each CPN will “callâ€? for one or more CCPNs capable of hybridization to the CPN. Following the formation of a supramolecular hybridization complex comprising a plurality of CPNs and a plurality of CCPNs, the reaction of reactive groups results in the formation of a molecule comprising covalently linked functional entities. The formation of the molecule involves the transfer of functional entities from one or more “donor CCPNsâ€? to at least one “acceptor CCPNâ€? with which the transferred functional entities were not associated prior to the transfer.

专利号:US-6175004-B1
优先权日:1998-09-01
标题 :Process for the synthesis of oligonucleotides incorporating 2-aminoadenosine
发明人：ROSS BRUCE S; MANOHARAN MUTHIAH
权利人:ISIS PHARMACEUTICALS INC
摘要:This invention presents novel processes for incorporating 2-aminoadenosine and 2-aminoadenosine analogs into oligonucleotides. A halogenated adeninosine is incorporated into an oligonucleotide using standard synthesis methods, such as phosphoramidited protocols. Subsequent reaction with an amine results in the desired product. The oligonucleotides produced provide stronger hybridization to their target sequences. These oligonucleotides can be useful compounds, inter alia for diagnostic and therapeutic applications.

专利号:US-9938282-B2
优先权日:2014-02-05
标 题:Expedient synthesis of sitagliptin
发明人：JANAGANI SATYANARAYANA; THADURI VENKATESHWAR KUMAR; VAMARAJU RAVISANKAR
权利人:STEREOKEM INC
摘要:Novel intermediates are disclosed as intermediates for preparation of a Sitagliptin. A novel synthetic method to prepare Sitagliptin using the said intermediates is also disclosed.

专利号:WO-2018115169-A1
优先权日:2016-12-21
标题 :Method for continuous polymerisation of diene elastomer with lithium amide initiator
发明人：DESSENDIER MARIE-HÉLÈNE; DIRE CHARLOTTE; FAUVARQUE-NUYTTEN CLAIRE
权利人:MICHELIN & CIE
摘要:The invention relates to a method for continuous synthesis of a diene elastomer by means of n reactors r1 to rn, provided with an internal stirring system, assumed to be perfectly stirred, arranged in series, n ranging from 2 to 15, preferably from 2 to 9, the reactor r1 being supplied with an input solution comprising a solvent, one or more monomers, an anionic polymerisation initiator chosen among the lithium amides and a polar agent, one or more reactors r2 to rn optionally also being supplied by re-injection of a purified solution comprising solvent and/or one or more monomers and/or polar agent, the temperature of each reactor ranging from 20°C to 150°C, preferably ranging from 30°C to 120°C and being no lower than the temperature of the reactor that immediately precedes same, the temperature of the reactor rn being higher than the temperature of the reactor r1, the diene elastomer obtained having a polymolecularity index ranging from 1.1 to 1.7.