SYNTHETIC INTERMEDIATE OF 6-(7-((1-AMINOCYCLOPROPYL)METHOXY)-6-METHOXYQUINOLIN-4-YLOXY)-N-METHYL-1-NAPHTHOAMIDE AND PHARMACEUTICALLY ACCEPTABLE SALT AND APPLICATION OF THE SAME
PROBLEM TO BE SOLVED: To provide a novel intermediate useful for preparation of 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthoamide, a compound useful in treatment of formation of a neogenetic tissue, with high yield and purity and its applications.SOLUTION: With e.g. 1-benzyloxycarbonylamino-1-((4-acetyl-2-methoxyphenoxymethyl)cyclopropane as a first intermediate, an intermediate with the p position of the methoxyphenyl nitrated, an intermediate with the acetyl group converted to an aminopropenoyl or an intermediate consisting of a compound of the following formula, with the nitro group reduced to a quinoline ring, is obtained. The target compound is obtained by methylaminocarbonylating the chloro group through an intermediate with the OH of the quinoline ring of the compound converted to a chloro group and removing the protective group.【課題】新生組織形成の治療に有用な化合物６－（７－（（１－アミノシクロプロピル）メトキシ）－６－メトキシキノリン－４－イルオキシ）－Ｎ－メチル－１－ナフトアミドを、高い収率及び純度で調製するために有用な新規中間体及びその使用を提供する。【解決手段】例えば、１－ベンジルオキシカルボニルアミノ-1-（（４－アセチル－２－メトキシフェノキシメチル）シクロプロパンを第一の中間体とし、メトキシフェニルのｐ位をニトロ化した中間体、アセチル基をアミノプロペノイルに変えた中間体、ニトロ基を還元しキノリン環とした中間体（下記式化合物）を得る。該化合物のキノリン環のＯＨがクロルに変わった中間体を経て、クロルをメチルアミノカルボニル化後、保護基を外し、目的化合物を得る。【選択図】なし
