醋酸叔丁酯置于乙醚,氨,Sodium Amide体系中,化学反应生成 叔丁基甲基马来酸酯 参考文献:Hauser; Levine; Kibler,Journal Of The American Chemical Society,1946,Vol. 68,P. 27 标题:Hauser; Levine; Kibler,Journal Of The American Chemical Society,1946,Vol. 68,P. 27
专利号:US-4283536-A 优先权日:1977-12-29 标 题:Preparation of vincadifformine and related derivatives 发明人:KUEHNE MARTIN E 权利人:UNIV VERMONT 摘要:This invention relates to the preparation of vincadifformine and related derivatives which are useful as starting material for the synthesis of among other alkaloids vincamine and other similar compounds possessing interesting psychopharmacologic properties. n A tetrahydro-β-carboline (II) is reacted with benzoyl chloride to provide a 2-benzoyl-1,2,3,4-tetrahydro-9H-pyrido-(3,4-b)-indole (III). Then compound (III) is reduced to give a 2-benzyl-1,2,3,4-tetrahydro-9H-pyrido-(3,4-b)-indole (IV). Thereafter, compound (IV) is transformed by t-butyl hypochlorite into a chloroindolenine derivative (V) which is immediately treated with a metal dialkylmalonate such as thallium t-butyl methyl malonate to give a dialkyl 3-benzyl-1,2,3,4,5,6-hexahydroazepino-(4,5-b)-indole-5,5-dicarboxylate (VI). Compound (VI) is then partly decarboxylated into a alkyl 3-benzyl-1,2,3,4,5,6-hexahydro-(4,5-b) indole-5-carboxylate (VII). Compound (VII) is hydrogenated to give an alkyl 1,2,3,4,5,6-hexahydroazepino-(4,5-b)-indole 5-carboxylate (VIII). In an alternative embodiment, compound (VI) can be hydrogenated to the corresponding dialkyl 1,2,3,4,5,6-hexahydroazepino-(4,5-b)-indole-5,5-dicarboxylate which is then decarboxylated into compound (VIII). Compound (VIII) is condensed with a functionalised aldehyde, typically a epoxy aldehyde or a haloaldehyde such as 1-bromo-4-formylhexane, to give vincadifformine or similar pentacyclic derivatives.
专利号:US-9693999-B2 优先权日:2011-01-26 标题:Small molecule RNase inhibitors and methods of use 发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE 权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education 摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.
专利号:US-9744252-B2 优先权日:2011-08-17 标 题:Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi 发明人:BERGER MARKUS; KRUGER MARTIN; LOHRKE JESSICA; REINHARDT MICHAEL; SIEBENEICHER HOLGER 权利人:PIRAMAL IMAGING SA 摘要:The present invention relates to novel fluorine containing compounds, methods for their preparation, the intermediates of the synthesis, their use as diagnostic agents, especially for imaging of thrombi. The invention relates to positron emission tomography (PET) agents and associated precursor reagents, and methods for producing such radiolaveled agents for imaging of thrombi in a mammalian body. More particularly, the invention relates to small nonpeptide, high-affinity, specific-binding glycoprotein IIb/IIIa antagonists for imaging of thrombi.
专利号:CN-113461679-B 优先权日:2021-06-29 标题 :Synthesis of a Benzazepine Isatin Compound
专利号:JP-2005104860-A 优先权日:2003-09-29 标题 :Synthesis of cyclic non-protein amino acids
专利号:EP-0224088-A2 优先权日:1985-11-28 标题 :Process for the solid-phase synthesis of retro-inverso peptides
参考标题:Rh(III)-Catalyzed Regio- And Chemoselective [4 + 1]-Annulation Of Azoxy Compounds With Diazoesters For The Synthesis Of 2H-Indazoles: Roles Of The Azoxy Oxygen Atom 作者:Zhen Long,Zhigang Wang,Danni Zhou,Danyang Wan,Jingsong You |发布日期:2017.6.2 摘要:Tandem C-H Alkylation/intramolecular Decarboxylative Cyclization Of Azoxy Compounds With Diazoesters For The Synthesis Of 3-Acyl-2H-Indazoles Is Disclosed. The Azoxy Instead Of The Azo Group Enables A Distinct Approach For Cyclative Capture, Leading To A [4 + 1]-Annulation Rather Than A Classic [4 + 2] Manner. The Azoxy Oxygen Atom Is Traceless After Annulation, And Further Removal From The Product Is