专利号:WO-2024062080-A1 优先权日:2022-09-21 标题:Improved synthesis of psilocybin derivatives 发明人:HAMMES CHRISTIAN; STÖCKLI STEFAN 权利人:CARBOGEN AMCIS AG; AAMANYA AG 摘要:The present invention relates to an improved synthesis of psilocybin and alkyl- derivatives of psilocybin such as ethocybin (4-phosphoryloxy-N,N-diethyltryptamine, also known as phosphoryloxy-DET, PO-DET or CEY-39) and furthermore, relates to intermediates useful in the synthesis of these compounds.
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-2016280691-A1 优先权日:2013-11-07 标 题 :Triazole intermediates useful in the synthesis of protected n-alkyltriazolecarbaldehydes 发明人:HENDERSON MARK 权利人:BIOMARIN PHARM INC 摘要:Described herein are compounds and methods of making such compounds useful in the synthesis of protected N-alkyl-triazolecarbaldehydes.
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-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.
专利号:US-10464958-B2 优先权日:2012-07-17 标题 :Method for the synthesis of alpha-aminoalkylenephosphonic acid 发明人:NOTTE PATRICK; COGELS SAMUEL; BURCK SEBASTIAN 权利人:MONSANTO TECHNOLOGY LLC 摘要:The present invention is related to a new method for the synthesis of alpha-aminoalkylenephosphonic acid or its phosphonate esters comprising the steps of forming a reaction mixture by mixing a P—O—P anhydride moiety comprising compound, having one P-atom at the oxidation state (+III) and the other P-atom at the oxidation state (+III) or (+V), an aminoalkanecarboxylic acid and an acid catalyst, wherein said reaction mixture comprises an equivalent ratio of alpha-aminoalkylene carboxylic acid to P—O—P anhydride moieties of at least 0.2, and recovering the resulting alpha-aminoalkylene phosphonic acid compound or an ester thereof from the reaction mixture.
摘要:Zaidlewicz, M.; Krzemiński, M. P.; Dzieleńdziak, A., Science of Synthesis, (2009) 48, 366. 摘要:Fowler, L. S.; Sutherland, A., Science of Synthesis Knowledge Updates, (2010) 3, 144. 摘要:Hollmann, F., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 3, 122. 摘要:Dong, X.; Qin, H.; Chen, Y., Science of Synthesis: Hypervalent Halogens in Organic Synthesis, (2025) .