CAS: 1068-90-2; Diethyl 2-Acetamidomalonate

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1-(5-[1-(2-Chlorobenzoyl)-Amino]-6-(4-Chlorophenylamino)-Pyrimidin-4-yl)-4-Ethylamino-Piperidine-4-Carboxamide 以84的收率获得乙酰氨基丙二酸二乙酯
参考文献: A Process For The Preparation Of An Intermediate For A Triazolopyrimidine Carbonucleoside[fr] Procédé Pour La Préparation D'Un Intermédiaire Pour Un Carbonucléoside De Triazolopyrimidine
标题: A Process For The Preparation Of An Intermediate For A Triazolopyrimidine Carbonucleoside[fr] Procédé Pour La Préparation D'Un Intermédiaire Pour Un Carbonucléoside De Triazolopyrimidine
摘要:一种制备式(II)的4,6-二卤嘧啶-5-胺或其盐的方法,包括将式(III)的5-氨基嘧啶-4,6-二醇或其盐,或者化合物式(III)或其盐的溶剂与卤代试剂反应,新的中间体有助于制备式(II)的化合物以及制备这些中间体的方法.该发明还涉及一种从式(iia)的4,6-二卤-2-(丙硫基)嘧啶-5-胺制备替卡格雷洛或其药学上可接受的盐的方法.

专利信息

专利号:US-11667658-B2
优先权日:2021-06-30
标 题:Chemical synthesis of the organoarsenical antibiotic arsinothricin
发明人：ROSEN BARRY P; YOSHINAGA MASAFUMI; WNUK STANISLAW F; HOWLADER MD ABU HASAN; SUZOL SK MD SAZZAD HOSSAIN
权利人:ROSEN BARRY P; YOSHINAGA MASAFUMI; WNUK STANISLAW F; HOWLADER MD ABU HASAN; SUZOL SK MD SAZZAD HOSSAIN; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES
摘要:The subject invention provides methods for the chemical synthesis of racemic arsinothricin (D,L-AST), the novel organoarsenical antibiotic. One is by condensation of the 2-chloroethyl(methyl)arsinic acid with acetamidomalonate, and the second involves reduction of the N-acetyl-protected derivative of hydroxyarsinothricin (AST-OH) and subsequent methylation of the resulting sodium salt of trivalent arsenic intermediate with methyl iodide. The enzyme AST N-acetyltransferase (ArsN1) was utilized to purify L-AST from racemic AST. This expedient chemical synthesis of AST provides a source of this novel antibiotic for future drug development.

专利号:US-10189803-B2
优先权日:2008-02-22
标题 :Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions
发明人：CHONG HYUN-SOON
权利人:CHONG HYUN SOON; ILLINOIS INSTITUTE OF TECH
摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.

专利号:US-2016031800-A1
优先权日:2013-03-14
标 题:Synthesis of chiral kynurenine compounds and intermediates
发明人：TRETYAKOV ALEXANDER; DROUET KEITH E; SANDERS WILLIAM
权利人:VISTAGEN THERAPEUTICS INC
摘要:Provided are methods for the synthesis of compounds including chiral kynurenine compounds, intermediates useful for the synthesis thereof, and related compounds. For example, methods are provided for the synthesis of L-4-chlorokynurenine.

专利号:US-5665598-A
优先权日:1994-04-13
标题:Synthesis of chiral N-protected-α-substituted-glycine free acids by zinc-mediated addition of organic halide to glycine cation equivalent
发明人：ABOOD NORMAN A; NOSAL ROGER A
权利人:SEARLE & CO
摘要:A method is described for synthesis of N-Boc-L-propargylglycine, a key intermediate used in the preparation of high-potency, orally-active renin inhibitors. This method involves reaction of an organic halide with a glycine cation equivalent, such as methyl N-Boc-2-acetoxyglycine, in the presence of zinc dust to give Boc-protected amino acid derivatives in high yield. Typically useful organic halides are allylic, benzylic and propargylic halides. Resolution of methyl N-Boc-propargylglycine with alpha -chymotrypsin provides N-Boc-L-propargylglycine in high yield.

专利号:US-4751315-A
优先权日:1985-10-18
标 题 :Process for the preparation of clausenamide
发明人：HARTWIG WOLFGANG
权利人:BAYER AG; CHINESE ACAD MED SCIENCE
摘要:A new synthetic route to clausenamide having the formula ##STR1## has been found. It has been found that a compound of the formula ##STR2## can be oxidized to provide the stereochemically correctly configured product, clausenamide. A number of new compounds useful in the total synthesis of clausenamide have also been found. These compounds have the general formula ##STR3## wherein R is ##STR4## and CH 2 OH.

专利号:US-6350882-B1
优先权日:1999-05-21
标题:Synthesis of substituted prolines
发明人：EMERSON KHATEETA; HO GUO-JIE
权利人:MERCK & CO INC
摘要:The instant invention is directed to a process for synthesizing substituted prolines, in particular, optically pure substituted prolines, which comprises the steps of:a) adding an unsubstituted or substituted proline alkali salt and an alkali halide to a solution of dialkylacylamidomalonate; andb) adding alpha, beta unsaturated aldehyde to produce an adduct.