专利号:US-2006264608-A1 优先权日:2001-08-03 标题 :Bi-directional synthesis of oligoguanidine transport agents 发明人:WENDER PAUL A; VANDEUSEN CHRISTOPHER L; PATTABIRAMAN KANAKA; PELKEY ERIN T; JESSOP THEODORE C 权利人:WENDER PAUL A; VANDEUSEN CHRISTOPHER L; PATTABIRAMAN KANAKA; PELKEY ERIN T; JESSOP THEODORE C 摘要:Synthesis routes that can be adapted to large scale synthesis of oligoguanidine compounds such as oligoarginine compounds are described which use a perguanidinylation step to convert a group of ω-amino groups to the corresponding guanidinyl groups. These compounds find utility as transport agents. Modified oligoguanidine compounds are also described.
专利号:US-8471010-B2 优先权日:2008-05-13 标题:Synthesis of dihydrothieno[3,2-d]pyrimidine diols 发明人:FRUTOS ROGELIO P; TAMPONE THOMAS G; MULDER JASON ALAN; KRISHNAMURTHY DHILEEPKUMAR; SENANAYAKE CHRIS H 权利人:FRUTOS ROGELIO P; TAMPONE THOMAS G; MULDER JASON ALAN; KRISHNAMURTHY DHILEEPKUMAR; SENANAYAKE CHRIS H; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to an improved process for the preparation of dihydrothieno[3,2-d]pyrimidine diols, and similar pyrimidine diols, that is efficient, high-yielding, and does not require expensive and potentially unstable intermediates. The diols are used as intermediates in the synthesis of pyrimidine compounds which inhibit PDE4, and are thus useful in the treatment of respiratory or gastrointestinal diseases and complaints, peripheral or central nervous system diseases and disorders, inflammatory conditions, and cancers.
专利号:US-2011105786-A1 优先权日:2009-11-02 标 题 :Creatinol o-phosphate and synthesis method thereof 发明人:ZHANG GUOJI; ZHANG JIASHU 权利人:TIANJIN TIANCHENG PHARMACEUTICAL CO LTD 摘要:A creatinol O-phosphate is formed by chemically reacting a creatinol sulfate of creatinol compound with sulfuric acid to form a protected creatinol sulfate as a transition state of the synthesis process of the creatinol O-phosphate, wherein the protected creatinol is further reacted with one of P 2 O 5 , CIPO 3 H 2 , and POCl 3 to form the creatinol O-phosphate. The method of producing the protected creatinol sulfate includes a step of adding sulfuric acid into a creatinol sulfate to form a protected creatinol sulfate as the protected functional group. Therefore, the creatinol O-phosphate is formed by the process including the steps of chemically reacting the protected creatinol sulfate with one of POCl 3 , CIPO 3 OH 2 , and P 2 O 5 to form a creatinol O-phosphate solution; and crystallizing the creatinol O-phosphate solution to obtain crystallized creatinol O-phosphate.
专利号:US-2014256987-A1 优先权日:2013-03-09 标 题 :Creatinol O-phosphate and synthesis method thereof 发明人:ZHANG GUOJI 权利人:ZHANG GUOJI; TIANJIN TIANCHENG PHARMACEUTICAL CO LTD 摘要:A creatinol O-phosphate is formed by chemically reacting a creatinol sulfate of creatinol compound with sulfuric acid to form a protected creatinol sulfate as a transition state of the synthesis process of the creatinol O-phosphate, wherein the protected creatinol is further reacted with one of P 2 O 5 , CIPO 3 H 2 , and POCl 3 to form the creatinol O-phosphate. The method of producing the protected creatinol sulfate includes a step of adding sulfuric acid into a creatinol sulfate to form a protected creatinol sulfate as the protected functional group. Therefore, the creatinol O-phosphate is formed by the process including the steps of chemically reacting the protected creatinol sulfate with one of POCl 3 , ClPO 3 OH 2 , and P 2 O 5 to form a creatinol O-phosphate solution; and crystallizing the creatinol O-phosphate solution to obtain crystallized creatinol O-phosphate.
专利号:US-2011105797-A1 优先权日:2009-11-02 标题:Creatinol sulfate and synthesis method thereof 发明人:ZHANG GUOJI; ZHANG JIASHU 权利人:TIANJIN TIANCHENG PHARMACEUTICAL CO LTD 摘要:A chemical compound of creatinol sulfate is formed by chemically reacting N-methyl-amino-ethanol, cyanamide, with sulfuric acid to produce the creatinol sulfate with relatively higher yield rate and purity, wherein the mol ratio of N-methyl-amino-ethanol, sulfuric acid, and cyanamide is approximately 2:1:2.
专利号:ES-2392920-T3 优先权日:2008-05-13 标 题:Synthesis of dihydrothiene [3,2-d] pyrimidine diols and similar pyrimidine diols
[参考文献]: Barbara T Alexander, Et Al. Inducible Nitric Oxide Synthase Inhibition Attenuates Renal Hemodynamics During Pregnancy. Hypertension. 2002 Feb;39(2 Pt 2):586-90. [参考文献]: J M Dick, Et Al. Influence Of Different Classes Of No Synthase Inhibitors In The Pig Gastric Fundus. Naunyn Schmiedebergs Arch Pharmacol. 1997 Oct;356(4):488-94. [参考文献]: J P Spiers, Et Al. Inotropic Response To Endothelin-1, Isoprenaline And Calcium In Cardiomyocytes Isolated From Endotoxin Treated Rats: Effects Of Ethyl-Isothiourea And Dexamethasone. Br J Pharmacol. 2000 Jul;130(6):1275-82. [参考文献]: Lianyi Lu, Et Al. Brain Neuronal/inducible Nitric Oxide Synthases And Cyclooxygenase-1 Are Involved In The Bombesin-Induced Activation Of Central Adrenomedullary Outflow In Rats. Eur J Pharmacol. 2008 Aug 20;590(1-3):177-84. [参考文献]: Lior Sasson, Et Al. Nitric Oxide Synthase Inhibitor (Mtr-105) During Open-Heart Surgery. A Pilot Double-Blind Placebo-Controlled Study Of Hemodynamic Effects And Safety. Cardiology. 2008;111(3):181-7.
合成参考文献
摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 166. 摘要:Yakugaku Zasshi. Journal of Pharmacy., 94(1419), 1974 [] 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).