摘要 |
1. The methanesulfonate of a camptothecin derivative, said methanesulfonate being represented by the following formula (1): or a hydrate thereof. 2. Pharmaceutical composition having antitumor activities, including camptothecin derivatives characterized in, that as said derivative it includes the methanesulfonate of a camptothecin derivative of formula (1) or its hydrate, or pharmaceutically acceptable salt. 3. Process for the preparation of the methanesulfonate of a camptothecin derivative, said methanesuifonate being represented by the following formula (1) which comprises treating, with methanesulfonic acid, a compound represented by the following formula (2) wherein X represents a protective group removable by methanesulfonic acid, and then subjecting the thus-treated compound to recrystailization. 4. A process for the preparation of the methanesulfonate of a camptothecin derivative, said methanesuifonate being represented by the following formula (1): which comprises protecting the amino group of a compound represented by the following formula (3): with a protecting group removable by methanesulfonic acid, treating with methanesulfonic acid and then subjecting the thus-treated compound to recrystallization. 5. A process according to Claims 4 or 5, wherein the protecting group removable by methanesulfonic acid is an acetyl group. 6. A process according to any one of Claims 4, 5 and 6, wherein a solvent used for recrystallization is a mixture of water and an alcohol. |
申请人 |
DAIICHI PHARMACEUTICAL CO., LTD.;KABUSHIKI KAISHA YAKULT HONSHA |
发明人 |
KAMIHARA, SHINJI;KAZUAKI, KANAI;SHIGERU, NOGUCHI;YIROFUMI, TERASAWA;HIROAKI, KITAOKA |