专利号:US-5760237-A 优先权日:1995-08-25 标 题 :Synthesis of l-azatyrosine using pseudoephedrine as a chiral auxiliary 发明人:MYERS ANDREW G 权利人:CALIFORNIA INST OF TECHN 摘要:A practical synthesis of the potential chemotherapeutic agent L-azatyrosine is described. The key step involved the alkylation of (R,R)-(-)-pseudoephedrine glycinamide with 5-benzenesulfonyloxy-2-iodomethylpyridine and proceeded in 70-95% yield and 89-95% de. Simultaneous hydrolysis of the auxiliary and the benzenesulfonate protecting group afforded L-azatyrosine of ≧99% ee in 73% yield on multigram scale (recovery yield of (R,R)-(-)-pseudoephedrine: 90%).
专利号:US-10954178-B1 优先权日:2020-08-28 标题 :Synthesis of haloindenes 发明人:WNUK STANISLAW F; HOWLADER MD ABU HASAN 权利人:WNUK STANISLAW F; HOWLADER MD ABU HASAN; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES 摘要:The subject invention provides an expedited synthesis of 5, 6, and 7-iodoindenes from the corresponding aminoindan-1-ones in more than 70% yield, employing readily available precursors and reagents. A three-step sequence involves diazotization-iodination of aminoindan-1-one followed by reduction and dehydration. The method has a general character and can be extended for the preparation of various 4-, 5-, 6- or 7-haloindenes using different halogen sources for diazotization-halogenation reaction.
专利号:WO-2013138200-A1 优先权日:2012-03-13 标 题 :Green chemistry synthesis of the malaria drug amodiaquine and analogs thereof 发明人:FORTUNAK JOSEPH MARIAN; KULKARNI AMOL ANANT; KING CHRISTOPHER 权利人:UNIV HOWARD 摘要:Methods are provided for a green chemistry one-pot synthesis of amodiaquine and amodiaquine analogs. The methods have a lower environmental impact, lower investment cost, reduced amounts of byproducts and impurities, and a shorter synthesis time, compared to current conventional synthesis methods. The methods reduce the total number of steps in the synthesis from four to five down to two, thereby simplifying production; and allow a reduced number of solvents and reagents to be used in production, thereby reducing the waste generated in the synthesis. The methods can reduce the waste to about 3-5 kilograms of waste generated per kilogram of product produced; and surprisingly improve the overall yield from 60-65% to greater than 90% as compared to the current conventional synthesis methods for amodiaquine and its analogs.
专利号:EP-0422090-B1 优先权日:1988-06-20 标 题:Derivatives of nucleosides which may be used for the synthesis of marked oligonucleotides, and oligonucleotides obtained from these derivatives and their synthesis 摘要:A nucleoside derivative which may be used for the synthesis of oligonucleotides of the formula (I), in which: R1 represents a hydrogen atom or an unstable radical in an acid medium suitable for nucleotide synthesis; R2 represents a hydrogen atom or a protective radical, a functional radical or a support which may be used for nucleotide synthesis; R3 represents a hydrogen atom, the hydroxyl radical or a protected hydroxyl radical; and B represents a radical derived from a puric or pyrimidic base comprising an exocyclic NH2 group substituted by an R4Z group where R4 represents a single bond or a hydrocarbonated radical and Z is a marker element.
专利号:US-2024309024-A1 优先权日:2023-03-14 标题 :Direct synthesis of alkenylhalosilanes 发明人:LEWIS KENRICK MARTIN; ZHU YANJUN; BYRNE CHRISTOPHER M 权利人:MOMENTIVE PERFORMANCE MAT INC 摘要:A process for the direct synthesis of alkenylhalosilane monomers. Forming a slurry of liquid and copper-activated silicon from fresh silicon, cyclone fines and/or fine dust from silicon grinding, ultrafines and/or spent contact mass from the Direct Synthesis of alkylhalosilanes and arylhalosilanes, in a thermally stable solvent. Reacting the silanes by agitating the slurry with at least one unsaturated aliphatic or cycloaliphatic organohalide of the formula R1X, and optionally an organohalosilane and/or hydrogen halide, in the presence of a polymerization inhibiting Lewis base additive, at a reaction time, temperature and pressure effective to produce alkenylhalosilanes having the formulae, R1SiHX2, R12SiHX, R13SiX, R1SiX3, and R12SiX2 or mixtures thereof.
专利号:US-2004018598-A1 优先权日:2000-05-30 标题 :Bio-intermediates for use in the chemical synthesis of polyketides 发明人:SANTI DANIEL; ASHLEY GARY; MYLES DAVID C 摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.
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