N-Methyl-N-Pentyl-Aminopropionic Acid Hydrochloride置于亚磷酸,三氯化磷,水体系中,用 甲苯 用作溶剂,化学反应生成伊班膦酸 参考文献:Process For The Synthesis Of Ibandronate Sodium 标题:Process For The Synthesis Of Ibandronate Sodium
专利号:WO-2011016738-A8 优先权日:2009-08-05 标 题 :A process for the synthesis of 1-hydroxy-3-(n-methylpentylamino) propylidene bisphosphonic acid monosodium salt, monohydrate 发明人:SZULC MARCIN; SLISEWSKI TOMASZ; DEMBKOWSKI LESZEK; JASTRZEBSKA BEATA; RACHON JANUSZ; MAKOWIEC SLAWOMIR 权利人:ZAKLADY FARMACEUTYCZNE POLPHARMA SA; POLITECHNIKA GDANSKA; SZULC MARCIN; SLISEWSKI TOMASZ; DEMBKOWSKI LESZEK; JASTRZEBSKA BEATA; RACHON JANUSZ; MAKOWIEC SLAWOMIR 摘要:A process for the synthesis of 1-hydroxy-3-(N-methylpentylamino) propylidene bisphosphonic acid monosodium salt, monohydrate which consists in the reaction of phosphorus trichloride with an aqueous solution of 3-(N-methylpentylamino)propionic acid hydrochloride at a temperature of 0-80°C, removing excess unreacted phosphorus trichloride, hydrolysis of the reaction mixture under reflux, conversion of 1-hydroxy-3-(N- methylpentylamino) propylidene bisphosphonic acid into its monosodium salt using sodium cation-containing alkaline substances, crystallisation using an anti-solvent. Also disclosed is a process for the synthesis of a polymorphic form of 1-hydroxy-3-(N-methylpentylamino) propylidene bisphosphonic acid monosodium salt, monohydrate which consists of initiating and carryout the crystallisation using acetone at a temperature of 0-5°C.
专利号:US-8178712-B2 优先权日:2006-06-23 标 题:Process for the synthesis of Ibandronate sodium 发明人:RAO DHARAMARAJ RAMCHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI GANPATI 权利人:RAO DHARAMARAJ RAMCHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI GANPATI; CIPLA LTD 摘要:The present invention relates to an improved process for the synthesis of Ibandronate sodium of formula (I). The present invention also provides novel processes for the synthesis of 3-[N-(methylpentyl)amino]propionic acid (III).
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-12391691-B2 优先权日:2018-11-16 标题:Synthesis of key intermediate of KRAS G12C inhibitor compound 发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY 权利人:AMGEN INC 摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as
专利号:US-2025206736-A1 优先权日:2019-11-14 标题 :Synthesis of kras g12c inhibitor compound 发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN 权利人:AMGEN INC 摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.
专利号:WO-2017100796-A1 优先权日:2015-12-11 标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI 权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.
1. McCormack PL, Plosker GL. Ibandronic acid: a review of its use in the treatment of bone metastases of breast cancer. Drugs. 2006;66(5):711-728. doi:10.2165/00003495-200666050-00011 2. Barrett-Lee P, Casbard A, Abraham J, et al. Oral ibandronic acid versus intravenous zoledronic acid in treatment of bone metastases from breast cancer: a randomised, open label, non-inferiority phase 3 trial [published correction appears in Lancet Oncol. 2014 Feb;15(2):e52-3]. Lancet Oncol. 2014;15(1):114-122. doi:10.1016/S1470-2045(13)70539-4
合成参考文献
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