甘氨酸酐 以 Acetic Anhydride (Ac2O),乙酸乙酯 作为反应溶剂,以26.4 G (61%)的收率获得产物1,4-二乙酰基哌嗪-2,5-二酮 参考文献:Dehydrophenylahistins And Analogs Thereof And The Synthesis Of Dehydrophenylahistins And Analogs Thereof 标题:Dehydrophenylahistins And Analogs Thereof And The Synthesis Of Dehydrophenylahistins And Analogs Thereof 摘要:公开了以下结构(i)代表的化合物:制备这种化合物的方法也被公开,其中所述方法包括将二酰基二酮哌嗪与第一醛反应以产生中间化合物;然后将中间化合物与第二醛反应,以产生具有通用结构的化合物类,其中第一醛和第二醛选自氧唑羧醛,咪唑羧醛,苯甲醛,咪唑羧醛衍生物和苯甲醛衍生物组成的群体,从而形成上述化合物,其中r1,R1',R1'',R2,R3,R4,R5和r6,X1和x2,Y,Z,Z1,Z2,Z3和z4可以分别根据附带说明书中的描述进行定义.还公开了用于治疗血管增殖的组合物和方法.
专利号:US-2004030209-A1 优先权日:2000-11-30 标 题:Method for the production of alkyl aryl sulphonates 发明人:NARBESHUBER THOMAS; STEINBRENNER ULRICH; KRACK GERHARD 摘要:The preparation of alkylaryl compounds takes place by n 1) preparation of a mixture of, on statistical average, predominantly monobranched C 10-14 -olefins by n a) reaction of a C 4 -olefin mixture over a metathesis catalyst for the preparation of an olefin mixture comprising 2-pentene and/or 3-hexene, and optional removal of 2-pentene and/or 3-hexene, followed by dimerization of the resulting 2-pentene and/or 3-hexene over a dimerization catalyst to give a mixture comprising C 10-12 -olefins, and optionally removal of the C 10-12 -olefins, or n b) extraction of predominantly monobranched paraffins from kerosene cuts and subsequent dehydrogenation, or n c) Fischer-Tropsch synthesis of olefins or paraffins, where the paraffins are dehydrogenated, or n d) dimerization of shorter-chain internal olefins, or n e) isomerization of linear olefins or paraffins, where the isomerized paraffins are dehydrogenated, n 2) reaction of the olefin mixture obtained in stage 1) with an aromatic hydrocarbon in the presence of an alkylation catalyst which contains zeolites of the faujasite type.
专利号:US-7935704-B2 优先权日:2003-08-01 标 题 :Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof 发明人:PALLADINO MICHAEL A; LLOYD GEORGE KENNETH; HAYASHI YOSHIO; NICHOLSON BENJAMIN 权利人:NEREUS PHARMACEUTICALS INC 摘要:Compounds represented by the following structure (I) are disclosed: n nas are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R 1 , R 1 ′, R 1 ″, R 2 , R 3 , R 4 , R 5 , and R 6 , X 1 and X 2 , Y, Z, Z 1 , Z 2 , Z 3 , and Z 4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating vascular proliferation are also disclosed.
专利号:US-7956058-B2 优先权日:2002-08-02 标 题:Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof 发明人:HAYASHI YOSHIO; PALLADINO JR MICHAEL A; GRODBERG JENNIFER 权利人:NEREUS PHARMACEUTICALS INC 摘要:Compounds represented by the following structure (I) are disclosed: n nas are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R 1 , R 1 ′, R 1 ′, R 2 , R 3 , R 4 , R 5 , and R 6 , X 1 and X 2 , Y, Z, Z 1 , Z 2 , Z 3 , and Z 4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating cancer and fungal infection are also disclosed.
专利号:US-8993762-B2 优先权日:2013-03-15 标题 :Total synthesis of thaxtomin A analogues and their intermediates 发明人:HUANG HUAZHANG; YAN DONG; XUE ZHIJIE; ZHANG HONGBO 权利人:MARRONE BIO INNOVATIONS INC; MARRONE BIO INNOVATIONS INC 摘要:Improved synthetic methods for the production of thaxtomin analogs, particularly thaxtomin A, and intermediates therefore such as substituted tryptophans and in particular, 4-nitro-L-tryptophan, and substituted phenyl acrylic acids are disclosed. Bioassays show that the synthetic thaxtomin A is not significantly different from the natural one in herbicidal activity.
专利号:US-10434098-B2 优先权日:2015-06-02 标 题 :Deuterated dehydrophenylahistin compounds and preparation method thereof and use thereof in preparation of anti-tumor drugs 发明人:LI WENBAO; SUN TIANWEN; WANG SHIXIAO; ZHAO JIANCHUN; CAI BING; GUAN HUASHI 权利人:MARINE BIOMEDICAL RES INST QINGDAO CO LTD 摘要:Provided are a deuterium-substituted dehydrophenylahistin-like compound, preparation method thereof and use in a preparation of antitumor drugs. The deuterium-substituted dehydrophenylahistin-like compound has a structure of general formula (I), and a synthesis method thereof comprises: firstly conducting a condensation reaction of diacetyldiketopiperazine and an aldehyde intermediate a or a deuterated aldehyde compound b to form a heterocyclic compound c or a deuterium-containing heterocyclic compound d, which is then subjected to a condensation reaction with benzaldehyde and a deuterium-substituted benzaldehyde-like compound to form the deuterium-substituted dehydrophenylahistin-like compound. Also provided are a highly effective deuterated aldehyde intermediate with a high deuterium substitution rate and a deuterium-containing heterocycle intermediate, and a synthesis method thereof. An experiment shows that the deuterium-substituted dehydrophenylahistin-like compound provided by the present invention has an effect on tubulin depolymerization and can treat a refractory solid tumor or lymphoma. The present invention provides a method for researching and developing antitumor drugs of the related compound.
专利号:US-2005197344-A1 优先权日:2003-08-01 标题 :Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
参考标题:Ir-Catalyzed Double Asymmetric Hydrogenation Of 3,6-Dialkylidene-2,5-Diketopiperazines For Enantioselective Synthesis Of Cyclic Dipeptides 作者:Yao Ge,Zhaobin Han,Zheng Wang,Kuiling Ding |发布日期:2019.6.5 摘要:Synthesis Of 6A And Efficient Construction Of Chiral Products 8, 14, And 17 As Well As A 2-Butenyl-Bridged Bicyclic Diketopiperazine 10 And Hydroxydiketopiperazine 11. With An Analogous Achiral Ir Catalyst, The Hydrogenation Of Enantiopure Monohydrogenated Intermediate 7A Gave Cis-6A As The Only Product, Indicating That The Second-Step Hydrogenation Of The Titled Transformation Is A Chiral Substrate Controlled
合成参考文献
参考文献:10.1055/s-0033-1340473 摘要:Liu Y, Liao S, Qin C, Yao P, Li J, Zhou X, Wang J, Huang Z. One-Pot Synthesis of Polysubstituted 3-Amino-2-oxo-2,7-dihydro-1H-azepines. Synthesis. 2014 Jan 02;46(05):621–8. doi: 10.1055/s-0033-1340473. 参考文献:10.1007/s11696-023-02742-2 摘要:Chen H, Liu Y, Jiang R, Yu X, Qin M, Gong P. Improved protocol for synthesizing (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylidene]piperazine-2,5-dione (plinabulin). Chem. Pap. 2023 Apr 08;77(7):3803–10. doi: 10.1007/s11696-023-02742-2.