专利名称 | Methyl {4, 6 - diamino -2 - [1 - (2 - fluorobenzyl) - 1H - 3, 4 a-b-pyrazolo : pyridine -3 - yl] pyrimidine -5 - yl} [...] pharmaceutically active compound is used as a method for purifying and method of preparation | ||
申请号 | JP2018128949 | 申请日 | |
公开(公告)号 | JP6514398B2 | 公开(公告)日 | |
申请(专利权)人 | アドヴェリオ・ファーマ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング | 发明人 | フランツ ヨーゼフ・マイス; ヨアヒム・レーゼ; ヴィンフリート・イェントゲン; コンラート・ジーゲル |
专利来源 | 国家知识产权局 | 转化方式 | |
摘要 |
Preparing (P1) methyl {4, 6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3, 4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate (I), involves cleavage of 2-[1-(2-fluorobenzyl)-1H-pyrazolo[3, 4-b]pyridin-3-yl]-5-[(E)-phenyldiazenyl]pyrimidine-4, 6-diamine by catalytic hydrogenation, and isolation of 2-[1-(2-fluorobenzyl)-1H-pyrazolo[3, 4-b]pyridin-3-yl]-4, 5, 6-pyrimidinetriamine without intermediate formation of salts. Preparing (P1) methyl {4, 6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3, 4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate (I), involves : either cleavage of 2-[1-(2-fluorobenzyl)-1H-pyrazolo[3, 4-b]pyridin-3-yl]-5-[(E)-phenyldiazenyl]pyrimidine-4, 6-diamine by catalytic hydrogenation, and isolation of 2-[1-(2-fluorobenzyl)-1H-pyrazolo[3, 4-b]pyridin-3-yl]-4, 5, 6-pyrimidinetriamine without intermediate formation of salts; or reactionof 2-[1-(2-fluorobenzyl)-1H-pyrazolo[3, 4-b]pyridin-3-yl]-4, 5, 6-pyrimidinetriamine with methyl chloroformate or dimethyl dicarbonate to give methyl 4, 6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3, 4-b]pyridin-3-yl]-5-pyrimidinylcarbamate via a pyridine-free reaction route. Independent claims are included for the following : (1) purifying methyl {4, 6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3, 4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate, involving dissolving crude methyl {4, 6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3, 4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate in dimethyl sulfoxide; isolating the resulting methyl {4, 6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3, 4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate sulfinyldimethane; and removing the dimethyl sulfoxide by boiling in a solvent; (2) new methyl {4, 6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3, 4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate sulfinyldimethane (II); and (3) methyl {4, 6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3, 4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate is prepared by the process (P1). ACTIVITY : Cardiovascular-Gen.; Cardiant; Antianginal; Vasotropic; Antiarrhythmic; Thrombolytic; Cerebroprotective; Thrombolytic; Antiarteriosclerotic; Antiasthmatic; Cytostatic; Endocrine-Gen.; Osteopathic; Ophthalmological; Hypotensive; Respiratory-Gen.; Uropathic. No biological data given. MECHANISM OF ACTION : Soluble guanylate cyclase stimulator. |
主管部门:海南中小企业服务 | 建设单位:海南商业联合会
版权所有:海南商业联合会 | 备案号:粤ICP备13083911号(ICP加挂服务)@2017