Title:
【発明の名称】N-アリールメチル-アジリジン誘導体、前記誘導体から得られる1,4,7,10-テトラアザシクロドデカン誘導体、および、中間体としてのN-アリールメチル-エタノールアミンのスルホン酸エステルの製造方法
Document Type and Number:
Japanese Patent JPH11511733
Kind Code:
A
Abstract:
Aziridines may be subjeted 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-arylmethylethanolamine-sulphonate sulphonate ester with a base. N-aryimethyl-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.
Inventors:
Messare, Lewis
Amara Singe, Gandhara
Ferman, Jere Douglas
Martyr, Martha
John Varadalajan
Vasilevskis, Janice
Amara Singe, Gandhara
Ferman, Jere Douglas
Martyr, Martha
John Varadalajan
Vasilevskis, Janice
Application Number:
JP52736796A
Publication Date:
October 12, 1999
Filing Date:
March 08, 1996
Export Citation:
Assignee:
Nycomd Salter, Inc.
University of Iowa Research Foundation
University of Iowa Research Foundation
International Classes:
A61K49/00; A61K49/06; C07C303/44; C07D203/08; C07D255/00; C07D257/02; C07D259/00; C07C305/06; (IPC1-7): C07D203/08; C07D257/02; C07D259/00
Attorney, Agent or Firm:
Hiroyuki Ikeuchi (2 outside)