CAS: 6298-85-7; 2-Amino-6-Hydrazinylpyrimidin-4(3H)-One

上下游产品

2-amino-6-chloro-4-pyrimidinol 6-chlorois°Cytosine 7-Amino-1H-pyrimido[4,5-c]pyridazin-5-one pyridazin-5(6H)-one7-amino-3-phenylpyrimido4,5-cpyridazin-5(6H)-one -3-(4-hydroxyphenyl)propionic acid2-(2-amino-1,6-dihydro-6-oxo-4-pyrimidinyl)hydrazono-3-(4-hydroxyphenyl)propionic acid cyclohexyl>benzoatemethyl 4-4-(2-amino-4(3H)-oxopyrimidin-6-yl)hydrazon°Cyclohexylbenzoate

📜2-氨基-6-氯-4-羟基嘧啶置于一水合肼体系中,用 水 作为反应溶剂,化学反应 1.5H,以90%的收率获得产物2-氨基-4-羟基-6-肼基嘧啶
参考文献:5,10-亚甲基四氢-5-脱氮磷酸及其类似物:合成和生物活性.
标题:5,10-亚甲基四氢-5-脱氮磷酸及其类似物:合成和生物活性.
摘要:据报道,5,10-亚甲基四氢叶酸(1)的稳定,刚性类似物5,10-亚甲基-5-脱氮基氢氢叶酸(2)的合成可能是胸苷酸合酶的抑制剂.通过从2-氨基-6-肼基-4-氧代嘧啶(10)和二乙基n-[4-(3-甲酰基-1-吡咯基)苯甲酰基]-的amino16的fisher-吲哚型环化obtained得到目标化合物. L-谷氨酸(15),然后催化还原产物17.类似地,对适当的前体11和12进行fisher-吲哚型环化的修饰得到非经典类似物3-氨基-7,8,9-三甲基-2H-吡咯并[3',4':4,5]吡啶并[2,3-D]嘧啶-1-一(4)和3-氨基-8-苄基-7,9-二甲基-2H-吡咯并[3',4':4,5]吡啶并[2,3-D]嘧啶-1-酮(5).目标化合物2及其芳香族前体18 和非经典类似物4被评估为manca人淋巴瘤细胞生长的抑制剂,也被评估为人二氢叶酸还原酶,人胸苷酸合酶,甘氨酰胺核糖核苷
DOI:10.1021/jm00098A013

专利信息

专利号:WO-2012127472-A1
优先权日:2011-03-22
标题:Process and intermediates for the preparation of preladenant and related compounds
发明人：MAROM EHUD; MIZHIRITSKII MICHAEL; RUBNOV SHAI
权利人:MAPI PHARMA LTD; MAROM EHUD; MIZHIRITSKII MICHAEL; RUBNOV SHAI
摘要:The present invention describes processes for the synthesis of 2-(furan-2-yl)-7-[2-[4-[4-(2-methoxyethoxy)phenyl]piperazin-l-yl] ethyl]-7H-pyrazolo[ 4,3-e ][1,2,4]- triazolo[1,5c] pyrimidin-5-amine (Preladenant) represented by the structure of formula (1 ), and solvates and salts thereof, especially salts with pharmaceutically acceptable acids. The process of the present invention is useful not only for Preladenant production, but also for the preparation of other biologically active compounds of general formula (17), such as A2a receptor antagonists used for the treatment of central nervous system diseases, among others. The present invention further relates to certain intermediates formed in such processes.