Dimethyl Aminomethylphosphonate Hydrochloride置于盐酸体系中,化学反应 8.0H,反应生成氨甲基膦酸 参考文献:Tritylamine (Triphenylmethylamine) In Organic Synthesis; I. The Synthesis Ofn-(Triphenylmethyl)Alkanimines,1-(Triphenylmethylamino)Alkylphosphonic Esters,And 1-Aminoalkylphosphonic Acids And Esters 标题:Tritylamine (Triphenylmethylamine) In Organic Synthesis; I. The Synthesis Ofn-(Triphenylmethyl)Alkanimines,1-(Triphenylmethylamino)Alkylphosphonic Esters,And 1-Aminoalkylphosphonic Acids And Esters 摘要:三甲胺(氨的合成类似物)在制备未知的n-(三苯甲基)烷基亚胺中的应用已被描述.这些亚胺是制备1-(三苯甲基氨基)烷基膦酸酯的便利合成子,后者可作为合成1-氨基烷基膦酸及其衍生物的起始材料. Doi:10.1055/s-1988-27576
专利信息
专利号:US-10040752-B2 优先权日:2015-08-24 标 题 :Synthesis of levomethadone hydrochloride or dextromethadone hydrochloride and methods for use thereof 发明人:MKRTCHYAN GNEL; YAO QINGWEI 权利人:CODY LABORATORIES INC 摘要:Highly efficient methods for synthesis of levomethadone hydrochloride or dextromethadone hydrochloride are provided starting from D-alanine, or L-alanine, respectively, with retention of configuration. Methods for treating a subject are provided comprising administering a composition comprising an effective amount of levomethadone hydrochloride having not more than 10 ppm dextromethadone.
专利号:US-10364262-B2 优先权日:2012-07-17 标 题 :Method for the synthesis of N-phosphonomethyliminodiacetic acid 发明人:DEVAUX ALBERT; BURCK SEBASTIAN; NOTTE PATRICK 权利人:MONSANTO TECHNOLOGY LLC 摘要:A method for synthesis of N-phosphonoalkyliminodiacetic acid or derivatives thereof by forming a reaction mixture having an acid catalyst, a compound of the following general formula R1—CH2—NX—CH2—R2 and a compound having one or more P—O—P anhydride moieties to form a compound having a formula R1—CH2—N(—CH2PO3R32)(—CH2—R2) wherein in R1—CH2—NX—CH2—R2: X is —CH2—OH or —CH2—COOH; R1 and R2 are independently selected from the group consisting of nitrile, C1-C4 alkyl carboxylate, and carboxylic acid for when X is —CH2—OH, or R1 and R2 are both carbonyl groups linked by a hydrogen substituted nitrogen atom or a C1-C4-alkyl substituted nitrogen atom; and R3 is H, an alkyl group, or an aryl group; the anhydride moieties in the P—O—P anhydride compound have one P atom at the oxidation state (+III) and one P atom at the oxidation state (+III) or (+V); and 2) hydrolyzing the mixture to form N-phosphonomethyliminodiacetic acid or one of its derivatives.
专利号:US-8314090-B2 优先权日:2008-11-06 标 题:Methods of synthesis of benzazepine derivatives 发明人:HOWBERT J JEFFRY; KUSUKUNTLA VENKAT REDDY; TRETYAKOV ALEXANDER; NIELSEN NATHAN; KRASIK PAVEL; JIANG JI-LONG; YANG HONG WOON 权利人:HOWBERT J JEFFRY; KUSUKUNTLA VENKAT REDDY; TRETYAKOV ALEXANDER; NIELSEN NATHAN; KRASIK PAVEL; JIANG JI-LONG; YANG HONG WOON; VENTIRX PHARMACEUTICALS INC; ARRAY BIOPHARMA INC 摘要:The disclosure describes method of synthesis of substituted benzazepine derivatives. Preferred methods according to the disclosure allow for large-scale preparation of benzazepine compounds having low levels of metal impurities. In some embodiments, preferred methods according to the disclosure also allow for the preparation of benzazepine derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. The methods disclosed herein find utility in synthetic organic chemistry as well as medicinal chemistry.
专利号:US-10280189-B2 优先权日:2012-07-17 标题:Method for the synthesis of aminoalkylenephosphonic acid 发明人:BURCK SEBASTIAN; LECLERCQ CEDRIC NICOLAS; NOTTE PATRICK 权利人:MONSANTO TECHNOLOGY LLC 摘要:A method for the synthesis of an aminoalkylenephosphonic acid or its phosphonate esters including the following steps: a) forming, in the presence of an aldehyde or ketone and an acid catalyst, a reaction mixture by mixing a compound having at least one HNR 1 R 2 moiety or a salt thereof, with a compound having one or more P—O—P anhydride moieties, the moieties having one P atom at the oxidation state (+III) and one P atom at the oxidation state (+III) or (+V), wherein the ratio of moles of aldehyde or ketone to N—H moieties is 1 or more and wherein the ratio of N—H moieties to P—O—P anhydride moieties is 0.3 or more, and b) recovering the resulting aminoalkylenephosphonic acid having compound or its phosphonate esters.
专利号:US-6518422-B2 优先权日:2001-04-18 标 题 :Process for the synthesis of (3aS)-5,5-dioxo-2,3,3a,4-tetrahydro-1H-pyrrolo[2,1-c][1,2,4] benzothiadiazine 发明人:FOUCHER ELSA; THOMINOT GILLES; LECOUVE JEAN-PIERRE; RAMSDEN JAMES ANDREW; COBLEY CHRISTOPHER JAMES 权利人:SERVIER LAB 摘要:Process for the industrial synthesis of (3aS)-5,5-dioxo-2,3,3a,4-tetrahydro-1H-pyrrolo[2,1-c][1,2,4]benzothiadiazine of formula (I):by enantioselective catalytic hydrogenation of 5,5-dioxo-2,3-dihydro-1H-pyrrolo[2,1-c][1,2,4]benzothiadiazine.
专利号:US-9676799-B2 优先权日:2012-07-17 标 题 :Method for the synthesis of N-(phosphonomethyl)glycine 发明人:BURCK SEBASTIAN; BRUYNEEL FREDERIC; NOTTE PATRICK 权利人:STRAITMARK HOLDING AG 摘要:A method for the synthesis of N-(phosphonomethyl)glycine or one of its derivatives selected from the group consisting of its salts, its phosphonate esters, or its phosphonate ester salts, which includes the steps of: a) forming, in the presence an acid catalyst, a reaction mixture having 2,5-diketopiperazine, formaldehyde and a compound including one or more P-0-P anhydride moieties, the moieties having one P atom at the oxidation state (+III) and the other P atom at the oxidation state (+III) or (+V), to form N,N′-bisphosphonomethyl-2,5-diketopiperazine, its mono- to tetra phosphonate esters, the dehydrated forms of N,N′-bisphosphonomethyl-2,5-diketopiperazine and the phosphonate esters of its dehydrated forms; and b) hydrolyzing the N,N′-bisphosphonomethyl-2,5-diketopiperazine, its dehydrated forms or their phosphonate esters to obtain N-(phosphonomethyl)glycine or one of its derivatives selected from the group consisting of its salts, its phosphonate esters and its phosphonate ester salts.
[参考文献]: Alyssa M A Toda, Et Al. Regulation Of Ampa Receptor Phosphorylation By The Neuropeptide Pacap38. Proc Natl Acad Sci U S A. 2015 May 26;112(21):6712-7. [参考文献]: David Baur, Et Al. Developmental Tightening Of Cerebellar Cortical Synaptic Influx-Release Coupling. J Neurosci. 2015 Feb 4;35(5):1858-71. [参考文献]: Eric M Prager, Et Al. Pathophysiological Mechanisms Underlying Increased Anxiety After Soman Exposure: Reduced Gabaergic Inhibition In The Basolateral Amygdala. Neurotoxicology. 2014 Sep:44:335-43. [参考文献]: Han-Jun Wang, Et Al. Glutamatergic Receptor Dysfunction In Spinal Cord Contributes To The Exaggerated Exercise Pressor Reflex In Heart Failure. Am J Physiol Heart Circ Physiol. 2015 Mar 1;308(5):H447-55. [参考文献]: Hannah C Bygd, Et Al. Altering In Vivo Macrophage Responses With Modified Polymer Properties. Biomaterials. 2015 Jul:56:187-97.
合成参考文献
参考文献:10.1107/s2052520620002917 摘要:Jha KK, Gruza B, Kumar P, Chodkiewicz ML, Dominiak PM. TAAM: a reliable and user friendly tool for hydrogen-atom location using routine X-ray diffraction data. Acta Crystallogr B Struct Sci Cryst Eng Mater. 2020 Jun 01;76(Pt 3):296–306. doi: 10.1107/s2052520620002917.