发明名称 |
PROCESS FOR THE PREPARATION OF PORPHYRIN DERIVATIVES AS ANTIMICROBIAL AGENTS BY PHOTODYNAMIC THERAPY (PDT) |
摘要 |
<p>There is provided a process for the preparation of 5,15-bis-[4-(3- trrmethylarnmonio-propyloxy)-phenyl]-porphyrin dihalide, wherein the process comprises step (a) of providing 4-(3-bromopropyloxy)benzaldehyde, step (b) of providing dipyrrolmethane, step (c) of reacting the 4-(3-bromopropyloxy)- benzaldehyde with the dipyrrol-methane, together with trifluoro acetic acid, in the presence of an oxidation reagent to produce 5,15-bis-[4-(3-bromo- propyloxy)-phenyl] -porphyrin which is purified by Soxhlet extraction from the adsorbed state on a bed of alumina under highly controlled conditions; and step (d) of reacting the 5,15-bis-[4-(3-bromo-propyloxy)-phenyl]-porphyrin with trimethylamine in the presence of dry dimethylformamide to produce 5,15-bis- [4-(3-trrmethylarnmonio-propyl-oxy)-phenyl] -porphyrin dibromide. In a preferred embodiment, the process further comprises step (e) of passing the 5, 15-bis-[4-(3 -1rimemylammonio-propyloxy)-phenyl]-porphyrin di-bromide produced in step (d) through an anion exchanger to produce 5,15-bis-[4-(3- trimethylammonio-propyloxy)-phenyl]-porphyrin dichloride. There is provided a process for the preparation of 5,15-bis-(4-{3-[(3-dimemylamino-propyl)- dimethyl-ammonio]-propyloxy} -phenyl] -porphyrin dihalide.</p> |
申请公布号 |
WO2007074340(A1) |
申请公布日期 |
2007.07.05 |
申请号 |
WO2006GB04920 |
申请日期 |
2006.12.22 |
申请人 |
DESTINY PHARMA LIMITED;SOLVIAS AG;BRUNDISH, DEREK;LOVE, WILLIAM;RHYS-WILLIAMS, WILLIAM;FENG, XIANG, DONG;NAUD, FREDERIC;MEIER, HANS |
发明人 |
BRUNDISH, DEREK;LOVE, WILLIAM;RHYS-WILLIAMS, WILLIAM;FENG, XIANG, DONG;NAUD, FREDERIC;MEIER, HANS |
分类号 |
C07D487/08;A61K31/409;A61P31/00;C07D487/22 |
主分类号 |
C07D487/08 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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