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:US-9376461-B2 优先权日:2011-06-06 标 题:Non-enzymatic synthesis of O-acetyl-ADP-ribose and analogues thereof 发明人:KOPPETSCH KARSTEN; SZCZEPANKIEWICZ BRUCE G; PERNI ROBERT B 权利人:KOPPETSCH KARSTEN; SZCZEPANKIEWICZ BRUCE G; PERNI ROBERT B; GLAXOSMITHKLINE LLC 摘要:Provided herein is a simple, one-step, non-enzymatic synthesis of O-Acetyl-ADP-ribose (OAADPR) from NAD and sodium acetate in acetic acid. The extension of this reaction to other carboxylic acids, demonstrates that the reaction between NAD, and NAD analogs produces mixtures of the corresponding 2′- and 3′-carboxylic esters. Included are O-carboxyl-ADP-ribose compounds and corresponding methods of synthesis (e.g., O-propionyl-ADP-ribose, O-succinyl-ADP-ribose, O-malonyl-ADP-ribose), as well as non-adenosine nucleoside compounds.
专利号:US-4870199-A 优先权日:1986-04-30 标题 :Processes for the synthesis of diprotected R[R*,S*]-3,5-dihydroxy-6-oxohexanoate esters 发明人:CHEN KAU-MING; HARDTMANN GOETZ E; KAPA PRASAD K; LEE GEORGE T; LINDER JEROME; WATTANASIN SOMPONG 权利人:SANDOZ PHARMACEUTICALS CORP 摘要:Process for the synthesis of compounds of the formula in R[R*,S*] enantiomeric form, wherein each P1 is independently an hydroxy group-protecting group, and R2z is C1-4alkyl, benzyl or allyl, comprising, as a key step when R2z is R2x, the reaction of the compound of the formula in (S) enantiomeric form with a compound of the formula Mg &cir& +2 ((-)OOC-CH2-COOR2x)2 to obtain a compound of the formula in (S) enantiomeric form, and, as a key step when R2z is R2y, the reaction of a compound of the formula in (S) enantioimeric form with a compound of the formula Li(+)(-)CH2-COOR2y to obtain a compound of the formula in (S) enantiomeric form, wherein R2x is primary or secondary C1-4alkyl, benzyl or allyl, R2y is C1-4alkyl not containing an asymmetric carbon atom, and R3' is methyl or ethyl, processes for the synthesis of compounds of the formula comprising reacting a compound of the formula with the reaction product of a strong base and a compound of the formula optionally followed by, when R2z is allyl, cleavage of the allyl and P1 groups to obtain the corresponding compound of the formula wherein each R7 is methyl or ethyl, R is as defined in the specification, and each P1 independently and R2z are as defined above, and the compounds of the formula wherein R and each R7 are as defined above.
专利号:US-2024294464-A1 优先权日:2021-10-27 标题 :Synthesis of restrained complexing agents 发明人:WONG NICHOLAS; GOSSELIN FRANCIS 权利人:GENENTECH INC 摘要:Improved methods of synthesis of a restrained complexing agent are described herein. Compounds, including salts and solvates thereof, and compositions relevant to the improved methods are also described.
专利号:US-2013150622-A1 优先权日:2011-12-12 标题:Stereoselective synthesis of tapentadol and its salts 发明人:FANDRICK DANIEL ROBERT; RODRIGUEZ SONIA; YANG BING-SHIOU 权利人:BOEHRINGER INGELHEIM INT; BOEHRINGER INGELHEIM INT 摘要:A process for the synthesis of a salt of tapentadol.
专利号:US-10604479-B2 优先权日:2013-11-18 标 题:Continuous process for the one-pot synthesis of metal salts and metal complexes 发明人:LEONARDI GIULIANO; GASPERONI GIOVANNI 权利人:VOLARE & CONNECTING LLC; LEONARDI GIULIANO; NOVUS INT INC 摘要:A continuous process is described for the one-pot synthesis of compounds, such as metal salts and metal complexes, as well as optionally for the protection of the compounds thus obtained by coating and/or impregnation with suitable compounds.
参考标题:Synthesis And Properties Of 2-Oxa-6-Azaspiro[3.3]Heptane Sulfonate Salts 作者:Richard Van Der Haas,Jeroen Dekker,Jorma Hassfeld,Anastasia Hager,Peter Fey,Philipp Rubenbauer,Eric Damen |发布日期:2017.6 摘要:2-Oxa-6-Azaspiro[3.3]Heptane Is Presented. While This Compound Is Often Isolated As An Oxalate Salt, Its Isolation As A Sulfonic Acid Salt Yields A More Stable And More Soluble Product. With These Improved Properties Access To A Wider Range Of Reaction Conditions With The Spirobicyclic 2-Oxa-6-Azaspiro[3.3]Heptane Has Been Enabled. An Improved Synthesis Of The Bicyclic Spiro Compound 2-Oxa-6-Azaspiro[3.3]Heptane Is
合成参考文献
参考文献:10.1007/s00248-011-9911-y 摘要:González-Arenzana L, López R, Santamaría P, Tenorio C, López-Alfaro I. Dynamics of indigenous lactic acid bacteria populations in wine fermentations from La Rioja (Spain) during three vintages. Microb Ecol. 2012 Jan;63(1):12–9. doi: 10.1007/s00248-011-9911-y.