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公开(公告)号：KR1020020003786A
公开(公告)日：2002-01-15
申请号：KR1020000038153
申请日：2000-07-05
Applicant: 한국화학연구원
IPC: C07D207/22
Abstract: PURPOSE: Provided is a method for preparing 3-methoxyimino-4-aminomethylpyrrolidine derivatives, which are used as a useful substituent for the position No.7 of quinolone antibiotics, from 1-benzyl-3-oxo-4-ethoxycarbo0nylpyrrolidine. CONSTITUTION: The method comprises the steps of: reacting a compound of the formula(2) with oxoamine compound or its salt to prepare a compound of the formula(3); reducing a compound of the formula(3) to prepare a compound of the formula(4); hydrogenating and amine-protecting the compound of the formula(4) to prepare a compound of the formula(5); sulfonating the compound of the formula(5) to prepare a compound of the formula(6); aminating or azidonating the compound of the formula(6) to prepare a compound of the formula(8a) or a compound of the formula(7) respectively; hydrogenating the compound of the formula(7) to prepare a compound of the formula(8a) or reacting the compound of the formula(6) with amide to prepare a compound of the formula(8b); and reacting the compound of the formula(8a) or (8b) with acid to deprotect amine.
Abstract translation: 目的：提供3-甲氧基亚氨基-4-氨基甲基吡咯烷衍生物作为喹诺酮类抗生素的第7位的有用取代基，由1-苄基-3-氧代-4-乙氧基羰基吡咯烷制备的方法。 方法：该方法包括以下步骤：使式（2）的化合物与氧代胺化合物或其盐反应以制备式（3）的化合物; 还原式（3）的化合物以制备式（4）的化合物; 氢化和胺保护式（4）化合物以制备式（5）化合物; 磺化式（5）化合物以制备式（6）化合物; 胺化或叠氮化式（6）化合物以分别制备式（8a）化合物或式（7）化合物; 氢化式（7）的化合物以制备式（8a）的化合物或使式（6）的化合物与酰胺反应以制备式（8b）的化合物; 并使式（8a）或（8b）的化合物与酸反应以使胺脱保护。
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公开(公告)号：KR100351659B1
公开(公告)日：2002-09-05
申请号：KR1020000038153
申请日：2000-07-05
Applicant: 한국화학연구원
IPC: C07D207/22
Abstract: 본 발명은 3-메톡시이미노-4-아미노메틸피롤리딘 유도체의 개선된 제조방법에 관한 것으로서, 1-벤질-3-옥소-4-에톡시카보닐피롤리딘으로부터 퀴놀론 항균제의 7번 위치의 유용한 치환기로 사용되는 하기 화학식 1의 3-메톡시이미노-4-아미노메틸피롤리딘 유도체를 간편하게 고효율로 제조할 수 있다:
상기 식에서,
R
1 은 수소, C
1-4 알킬기, 또는 아릴 또는 헤테로아릴기로 치환된 C
1-4 알킬기이고;
R
2 는 수소, C
1-4 알킬기, 포르밀기 또는 t-부톡시카보닐기이고;
HX는 유기산 또는 무기산을 나타내고;
n은 1 내지 3의 정수이다.
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