CAS: 918633-87-1; 2-Bromo-N-[(2-Bromoethylamino)-[(3-Methyl-2-Nitroimidazol-4-yl)Methoxy]Phosphoryl]Ethanamine

上下游产品

(3-甲基-2-硝基-3H-咪唑-4-基)-甲醇 (1-Methyl-2-Nitro-1H-Imidazol-5-yl)Methanol 39070-14-9
3-甲基-2-硝基-3H-咪唑-4-甲酸乙酯 Ethyl 1-Methyl-2-Nitro-1H-Imidazole-5-Carboxylate 39070-13-8

📜3-甲基-2-硝基-3H-咪唑-4-甲酸乙酯置于偶氮二甲酸二异丙酯,水,三乙胺,三苯基膦,Sodium Hydroxide体系中,用 四氢呋喃 作为反应溶剂,化学反应 2.0H,反应生成 Th 302; N,N'-双(2-溴乙基)二氨基膦酸 (1-甲基-2-硝基-1H-咪唑-5-基)甲酯
参考文献: Th-302 Solid Forms And Methods Related Thereto[fr] Formes Solides De Th-302 Et Procédés Associés
标题: Th-302 Solid Forms And Methods Related Thereto[fr] Formes Solides De Th-302 Et Procédés Associés
摘要:本发明提供了一种制备th-302及其固态形式的新方法.该化合物的固态形式是一种有效的抗癌剂,并可用于各种制药组合物中,特别适用于治疗癌症.本发明还提供了一种制备这种化合物和形式以及治疗哺乳动物癌症的方法,包括给予治疗有效量的th-302固态形式.

专利信息

专利号:US-2025011348-A1
优先权日:2023-06-13
标题:Synthesis Process of X-IPM, Stable Crystal Form and Application Thereof
发明人：DUAN JIANXIN; LU ZHAOQIANG; CAI XIAOHONG; FAN JINWEI; QIN WEI; HUANG QUNHUI; ZHANG YANJUN; CHEN WEISU
权利人:ASCENTAWITS PHARMACEUTICALS LTD
摘要:The present application relates to a new method for synthesizing isophosphoramide nitrogen mustard (X-IPM) that is suitable for industrialized production, involves fewer types of solvents, and leads to stable products with high yield. This method is charazterized mainly by the batchwise addition of M (e.g., M is R3N with R being ethyl; i.e., M is triethylamine) and the specific post-reaction treatment, which make it possible for the reaction to fully proceed, lead to products with less impurities, high yield and relatively stable properties, and can lead to stable crystallized substances with specific crystal structures. The present application also relates to stable crystal forms of the isophosphoramide nitrogen mustard (X-IPM) prepared by the aforementioned method, and use of the same as reactants for the synthesis of aziridine structure-containing compounds.

专利号:US-2016251387-A1
优先权日:2013-10-10
标 题:Synthesis of 1-alkyl-2-amino-imidazol-5-carboxylic acid ester via calpha-substituted n-alkyl-glycine ester derivatives
发明人：JASPER CHRISTIAN; HAHN HELMUT DIETER; BREUNING MARCEL ANDRE; KRATTIGER PHILIPP; DEBOR MICHAELA
权利人:MERCK PATENT GMBH
摘要:The invention provides an efficient and high yielding process for preparing TH-302, comprising at least one step wherein a dioxolane intermediate is generated in an aqueous layer, resulting in a synthesis that is amenable to scale up conditions.

专利号:US-2024425461-A1
优先权日:2023-06-13
标题 :Preparation process of intermediate, synthesis process of amino imidazole carboxylate ester and hplc purity measure method
发明人：DUAN JIANXIN; LU ZHAOQIANG; FAN JINWEI; HUANG QUNHUI; ZHANG YANJUN; CHEN WEISU; QIN WEI
权利人:ASCENTAWITS PHARMACEUTICALS LTD
摘要:This invention relates to a process for preparing an intermediate of aminoimidazole carboxylate, a process for synthesizing aminoimidazole carboxylate and an HPLC method for determining purity. The process of preparing the intermediate of aminoimidazole carboxylate comprises subjecting a compound of formula I-2 and a formate as the reactants to a first-step reaction in a benzene solvent and at a temperature of −5° C.−5° C., with the addition of a solution of sodium alkoxide in such a way that the temperature of the reaction solution is not higher than 5° C., to obtain the intermediate of aminoimidazole carboxylate or a mixture comprising a compound of formula I-3, i.e., the intermediate of aminoimidazole carboxylate. By using a sodium alkoxide reagent, as a comparatively safe alternative to NaH and potassium tert-butoxide which are prone to cause fire hazards or explosions and are not suitable for use in large-scale production, the process of the present application can ensure smooth progression of the reaction to the product and effectively improve the overall safety of the reaction without noticeably impairing the reaction efficiency.

专利号:US-2024208898-A1
优先权日:2021-03-25
标 题 :Enamine n-oxides: synthesis and application to hypoxia-responsive prodrugs and imaging agents
发明人：KIM JUSTIN; KANG DAHYE; CHEUNG SHELDON T
权利人:DANA FARBER CANCER INST INC
摘要:Disclosed are compounds and pharmaceutically acceptable salts and stereoisomers thereof that are suitable for diagnosis and the treatment of diseases and disorders characterized by, associate with or which exhibit tissue hypoxia, such as, for example, solid tumors. Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds.

专利号:WO-2015051921-A1
优先权日:2013-10-10
标题:Synthesis of 1-alkyl-2-amino-imidazol-5-carboxylic acid ester via calpha-substituted n-alkyl-glycine ester derivatives

专利号:CN-116789558-A
优先权日:2022-03-18
标题:Preparation method of intermediate, synthesis method of amino imidazole carboxylate and HPLC (high performance liquid chromatography) purity detection method