专利号:US-7893286-B2 优先权日:2007-06-01 标题 :Method for the synthesis of phospholipid ethers 发明人:PINCHUK ANATOLY; WEICHERT JAMEY P; LONGINO MARC 权利人:CELLECTAR INC 摘要:Disclosed are improved methods for the synthesis of phospholipid ether analogs and alkyl phosphocholine analogs. The methods allow greater versatility of the reactants used and greater ease in synthesizing alkyl chains of varying length while affording reaction temperatures at room temperature or below. The methods disclosed herein provide reactants and conditions using alkyl halides and organozinc reagents and do not utilize Gringard reactions thus, allowing greater ease of their separation and purity of products. The PLE compounds synthesized by the methods disclosed herein can also be used for synthesizing high specific activity phospholipid ether (PLE) analogs, for use in treatment and diagnosis of cancer.
专利号:WO-2025104624-A1 优先权日:2023-11-14 标题 :Synthesis of 1,5-anhydro-3-({5-chloro-4-[4-fluoro-2-(2-hydroxypropan-2-yl)-1-(propan-2-yl)-1h-benzimidazol-6-yl]pyrimidin-2-yl}amino)-2,3-dideoxy-d-threo-pentitol 发明人:ALEXANDER KATY LOUISE; ANSARI ZARRIN FAZAL KHADIJA; DANIELS DAVID SYDNEY BERNARD; HASSEL LUKE HARRY; KEEN STEPHEN PHILIP; SCOTT JEREMY PETER; SCOTT REUBEN JOHN; SIMMONS JOHATHAN ANDREW; STOLL EMMA LOUISE; TRINDADE ALEXANDRE FONSECA; VICINI ANNA CHIARA 权利人:PFIZER 摘要:This disclosure relates novel methods to prepare 1,5-anhydro-3-({5-chloro-4-[4- fluoro-2-(2-hydroxypropan-2-yl)-1-(propan-2-yl)-1H-benzimidazol-6-yl]pyrimidin-2- yl}amino)-2,3-dideoxy-D-threo-pentitol, and hydrates and stereoisomers thereof, as well as intermediates, including solid forms of the intermediates, useful for the preparation of such compounds and the synthesis of said intermediates.
专利号:US-2024010638-A1 优先权日:2020-11-13 标题:Improved synthesis of crac channel inhibitors 发明人:STAUDERMAN KENNETH; DUNN MICHAEL; OLMSTEAD KAY 权利人:CALCIMEDICA INC 摘要:Provided herein is an improved synthetic method for the production of CRAC channel inhibitors. The synthetic method provides a method for producing highly pure CRAC channel inhibitors for clinical testing.
专利号:EP-2647639-A1 优先权日:2012-04-06 标题:ß-boration of alkene and alkyne intermediates 权利人:LEK PHARMACEUTICALS 摘要:The present invention relates to the field of organic chemistry, and in particular to the preparation of β-borated compounds. These β-borated compounds can be used as intermediates in the synthesis of pharmaceutically active agents such as Sitagliptin.
专利号:US-9718807-B2 优先权日:2012-06-05 标 题 :Synthesis of antiviral compound 发明人:SCOTT ROBERT WILLIAM; VITALE JUSTIN PHILIP; MATTHEWS KENNETH STANLEY; TERESK MARTIN GERALD; FORMELLA ALEXANDRA; EVANS JARED WAYNE 权利人:GILEAD PHARMASSET LLC 摘要:The present disclosure provides processes for the preparation of a compound of formula I: n nwhich is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula I.
专利号:US-8022235-B2 优先权日:2007-06-01 标 题 :Compositions of phospholipid ether boronic acids and esters and methods for their synthesis and use 发明人:PINCHUK ANATOLY; WEICHERT JAMEY P; LONGINO MARC 权利人:CELLECTAR INC 摘要:The present invention discloses boronic acids and esters of phospholipid ether analogs and methods for their synthesis and use. The boronic acids and esters of phospholipid ether analogs described herein can be used in treating cancer and in particular can be used in conjunction with radiation therapy, such as external beam radiation therapy and neutron capture therapy to specifically target and kill cancer cells.
摘要:Podlech, J., Science of Synthesis Knowledge Updates, (2018) 4, 148. 摘要:Murata, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 440. 摘要:Yoshida, H., Science of Synthesis: Advances in Organoboron Chemistry towards Organic Synthesis, (2019) 1, 31. 摘要:Pineschi, M.; Boldrini, C., Science of Synthesis: Advances in Organoboron Chemistry towards Organic Synthesis, (2019) 1, 202. 摘要:Xu, L., Science of Synthesis: Advances in Organoboron Chemistry towards Organic Synthesis, (2019) 1, 273.