5-{4-[2-(5-Ethylpyridin-2-yl)-2-Hydroxyethoxy]Benzylidene}-2,4-Thiazolidene Dione置于哌啶,盐酸,Sodium Tetrahydroborate,N-溴代丁二酰亚胺(Nbs),氯化亚砜,Cobalt(II) Chloride Hexahydrate,Palladium 10% On Activated Carbon,水,氢气,Potassium Carbonate,溶剂黄146,二甲基乙二醛肟,三乙胺,锌体系中,用 甲醇,乙醇,二氯甲烷,氯仿,水,二甲基亚砜,N,N-二甲基甲酰胺,甲苯,叔丁醇 用作溶剂,-5.0~130.0 °C,413.7 Kpa 条件下,反应 55.67H,反应生成盐酸吡格列酮 参考文献:Novel Process To Prepare Pioglitazone Via Several Novel Intermediates 标题:Novel Process To Prepare Pioglitazone Via Several Novel Intermediates 摘要:一种制备噻唑烷二酮类药物的新工艺,首选为吡格列酮.还描述了参与其合成的新中间体,以及用于它们的制备和在医药中的应用的工艺.
专利号:WO-2009148195-A1 优先权日:2008-06-02 标题:5-(4-hydroxybenzyl)thiazolidine-2,4-dione as intermediate for synthesis of thiazolidinedione based compounds and process for preparing the same 发明人:PARK JIN OH; KIM YONG GIL; SON HAN IL; LEE YUN JEONG; KIM EUN MI 权利人:DAEBONG LS LTD; PARK JIN OH; KIM YONG GIL; SON HAN IL; LEE YUN JEONG; KIM EUN MI 摘要:The present invention relates to 5-(4-hydroxybenzyl)thiazolidine-2,4-dione represented by the following Chemical Formula [1], which is useful as an intermediate for synthesis of thiazolidinedione based compounds, a method for preparing the compound, and a method for preparing pioglitazone or pioglitazone hydrochloride, which is a thiazolidinedione based drug and useful in treating and preventing diabetes, using the 5-(4-hydroxybenzyl)thiazolidine-2,4-dione represented by Chemical Formula [1] as an intermediate:
专利号:EP-1694646-B1 优先权日:2003-12-19 标题 :Process for the synthesis of pioglitazone hydrogen chloride 发明人:FISCHER JANOS; FODOR TAMAS; LEVAI SANDOR; PETENYI ENDRENE; PERENYI EVA 权利人:RICHTER GEDEON VEGYESZET 摘要:The invention relates to a process for the synthesis of pioglitazone hydrogen chloride - which is an antidiabetic drug - via novel intermediates by reacting 4-[2-(5-ethyl-2-pyridinyl)-ethoxy]-benzaldehyde salt of formula (II), wherein HX is: HCI, CF3COOH, C4H4O4, (COOH)2 with a base and then thiazolidine-2,4-dione, and the obtained 5-[[4-[2-(5-ethyl-2-pyridinyl)ethoxy]phenyl]methylene]-2,4-thiazolidinedione base is treated with hydrochloric acid and the obtained 5-[[4-[2-(5-ethyl-2-pyridinyl)ethoxy]phenyl] methylene]-2,4-tiazolidinedione hydrogen chloride of formula(III) is hydrogenated in the presence of a catalyst. Further objects of the invention are the salts of general formula (II) and the benzylidene derivative of formula (III).
专利号:US-2025235415-A1 优先权日:2022-02-23 标 题:Modulation of human breast milk composition 发明人:ROSS MICHAEL G; DESAI MINA 权利人:LUNDQUIST INST FOR BIOMEDICAL INNOVATION AT HARBOR UCLA MEDICAL CENTER 摘要:Compositions and methods for improving a child, such as an infant's health, are provided. The methods entail improving the quality of breast milk in a female human individual that provides breast milk, or expects to provide breast milk, to the child, by administering to the individual an agent that increases the individual's sensitivity to insulin, and/or an agent that reduces the substrate uptake, synthesis or secretion of long chain fatty acids, reduces the substrate uptake, synthesis or secretion of short chain fatty acids, increases the amino acid uptake, protein synthesis or protein secretion of proteins, or reduces the uptake or synthesis of lactose.
专利号:US-11767317-B1 优先权日:2020-06-30 标题:Methods of synthesizing enantiopure deuterium-enriched pioglitazone 发明人:NAVARRE LAURE FRANÇOISE VALÉRIE; JACQUES VINCENT; BOLZE SÉBASTIEN 权利人:POXEL SA 摘要:The invention provides methods of synthesis of enantiopure deuterium enriched R-pioglitazone with structure of compound (IV), or a pharmaceutically acceptable salt thereof: n nThe invention further provides chemical intermediates useful in the synthesis of compound (IV), and methods of synthesizing those intermediates.
专利号:US-2017247359-A1 优先权日:2014-09-05 标题 :Process for the preparation of canagliflozin 发明人:VELLANKI SIVA RAM PRASAD; BALUSU RAJA BABU; PILLI RAMAKRISHNA; JAWAJI RAJESWARA ROA; ANNADASU ANKAMA NAYUDU 权利人:MYLAN LABORATORIES LTD 摘要:A process for the preparation of canagliflozin. The process may be effectively implemented on an industrial scale. Several compounds useful as intermediates for the synthesis of canagliflozin (Formula 4, Formula 4a, Formula 4b and Formula 5) are also disclosed. The process involves the reduction of the compound of formula 3 in the presence of a metal hydride and an organic solvent to obtain the compound of formula 4, converting this into a compound of formula 5 which in turn is converted into canagliflozin.
专利号:US-2025223262-A1 优先权日:2022-03-31 标 题 :Synthesis of morphinans with reduced herg activity and mop binding 发明人:LAMMERT ECKHARD; SCHOLZ OKKA; OTTER SILKE; HEREBIAN DIRAN; HOFFMANN TORSTEN; SANZ MIGUEL ANGEL; KRAMP LAURENZ; LEVY LAURA MARIANA; HRISTEVA STANIMIRA 权利人:HEINRICH HEINE UNIV DUESSELDORF; DEUTSCHE DIABETES FORSCHUNGSGESELLSCHAFT E V; TAROS CHEMICALS GMBH & CO KG 摘要:The invention relates to morphinan-derivatives, processes for their preparation, medicaments containing them and the use of these morphinan-derivatives for the preparation of medicaments.
1: Akabari AH, Gajiwala H, Patel SK, Surati J, Solanki D, Shah KV, Patel TJ, Patel SP. Stability-Indicating TLC-Densitometric and HPLC Methods for Simultaneous Determination of Teneligliptin and Pioglitazone in Pharmaceutical Dosage Forms with Eco-Friendly Assessment. J Chromatogr Sci. 2024 Jun 5:bmae038. doi: 10.1093/chromsci/bmae038. Epub ahead of print. 2023:2096521. doi: 10.1155/2023/2096521.
合成参考文献
参考文献:10.1007/s11130-011-0243-3 摘要:Kim D, Han GD. Ameliorating effects of fermented rice bran extract on oxidative stress induced by high glucose and hydrogen peroxide in 3T3-L1 adipocytes. Plant Foods Hum Nutr. 2011 Sep;66(3):285–90. doi: 10.1007/s11130-011-0243-3. 参考文献:10.3275/7865 摘要:Ren X, Wei Q, Shao H, Sun Z, Liu N. A rat model of diabetic artery calcification. Journal of Endocrinological Investigation. 2011 Jul 12;35(5):497–503. doi: 10.3275/7865. 参考文献:10.1186/1475-2840-10-65 摘要:Hanefeld M, Pfützner A, Forst T, Kleine I, Fuchs W. Double-blind, randomized, multicentre, and active comparator controlled investigation of the effect of Pioglitazone, Metformin, and the combination of both on cardiovascular risk in patients with type 2 diabetes receiving stable basal insulin therapy: the PIOCOMB study. Cardiovascular Diabetology. 2011 Jul 14;10(1):65. doi: 10.1186/1475-2840-10-65. 参考文献:10.1186/1475-2840-10-66 摘要:Tschöpe D, Bramlage P, Binz C, Krekler M, Plate T, Deeg E, Gitt AK. Antidiabetic pharmacotherapy and anamnestic hypoglycemia in a large cohort of type 2 diabetic patients - an analysis of the DiaRegis registry. Cardiovascular Diabetology. 2011 Jul 14;10(1):66. doi: 10.1186/1475-2840-10-66. 参考文献:10.1007/s10354-011-0914-6 摘要:Lechleitner M. Oral antidiabetic drug therapy in type 2 diabetes mellitus - focus on elderly patients. Wien Med Wochenschr. 2011 Jun;161(11-12):297–9. doi: 10.1007/s10354-011-0914-6.