发明名称 |
Preparation of N-arylmethyl aziridine derivatives, 1,4,7,10-tetraazacyclododecane derivatives obtained therefrom and N-arylmethyl-ethanol-amine sulphonate esters as intermediates |
摘要 |
PCT No. PCT/GB96/00552 Sec. 371 Date Dec. 2, 1997 Sec. 102(e) Date Dec. 2, 1997 PCT Filed Mar. 8, 1996 PCT Pub. No. WO96/28420 PCT Pub. Date Sep. 19, 1996Aziridines may be subjected to a cyclooligomerization reaction to produce polyazacycloalkane compounds useful for example in the preparation of chelating agents for use in diagnostic imaging contrast agents. N-benzyl-aziridine in particular is useful as it can be cyclotetramerized and debenzylated to yield cyclen, a key intermediate in chelating agent preparation. The invention provides a particularly attractive route to production of N-benzyl and other N-arylmethyl aziridines of formula (I) where each R1 is independently hydrogen or a group AR and Ar is an optionally substituted phenyl group. The process comprises reacting a purified N-arylmethylethanolaminesulphonate ester with a base. N-arylmethyl-ethanolamine sulphonate ester of the formula R'NHCH2CH2OSO3H, wherein the N-arylmethyl group R' is an N-(bisarylmethyl) or N-(triarylmethyl) group, as intermediates. In a further aspect, the invention provides compounds of formula (II) where Ar and R1 are as hereinabove defined and at least two differing ArCHR21 moieties are present.
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申请公布号 |
US6048979(A) |
申请公布日期 |
2000.04.11 |
申请号 |
US19970894790 |
申请日期 |
1997.12.02 |
申请人 |
NYCOMED SALUTAR, INC.;UNIVERSITY OF IOWA FOUNDATION |
发明人 |
VASILEVSKIS, JANIS;VARADARAJAN, JOHN;GARRITY, MARTHA;FELLMANN, JERE DOUGLAS;MESSERLE, LOUIS;AMARASINGHE, GANDARA |
分类号 |
A61K49/00;A61K49/06;C07C303/44;C07C305/06;C07D203/08;C07D255/00;C07D257/02;C07D259/00;(IPC1-7):C07D255/02;C07D203/06;C07D203/14 |
主分类号 |
A61K49/00 |
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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