Chong Kun Dang Corporation

Dong-A Pharmaceutical Co., Ltd

Kwang Dae Ok

Jong Min Kim

Sang Sup Jew

Myoung Goo Kim

Jeong Mi Hah

Hee Soon Lee

Kyeong Hoi Cha

Kwang Kyun Lee

Joon Kyum Kim

Hee Jin Kim

Dong Y Jung

Moon S Kim

Camptothecin derivatives and pharmaceutically acceptable salts thereof, its manufacturing method and an antineoplastic agent containing it. The camptothecin derivatives are modified in B-ring and E-ring and show improved water solubility and enhanced antineoplastic effect.

Camptothecin compounds and a method of preparation thereof

Intermediates for the synthesis of camptothecin of the formula II

Intermediates for the synthesis of camptothecin derivatives

The present invention relates to a L-talopyranoside derivative of the formula (I): ##STR1## wherein, A is hydrogen atom, a lower alkyl group having 1 to 5 carbon atoms, or a hydroxyl-protecting group; B.sub.1 and B.sub.2, the same or different from each other, are independently hydrogen atom or a hydroxyl-protecting group; R.sub.1 and R.sub.2 may form a alkylene group with a carbon atom of 5-position of the sugar skeleton, or one of them is hydrogen atom and the other is CH.sub.2 X wherein, X is hydrogen, or a protected or un-protected hydroxyl group. Provided that, the following compounds are excepted: ##STR2## wherein, B.sub.1 and B.sub.2 are independently hydrogen atom or acetyl. L-talopyronoside derivatives of the present invention is a very useful intermediate for the synthesis of anthracycline antibiotics having an antitumor activity. The process according to the invention has an advantage of significant reduction in the production cost and therefore expected to be very useful for the preparation of anthracycline antibiotics in an industrial scale.

L-talopyranoside derivatives and process for the preparation of same

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Suwon, South Korea

Kwang Dae Ok