Aminotetralone derivatives and preparation process thereof
AssigneesDaiichi Pharmaceutical Co., Ltd., Kabushiki Kaisha Yakult Honsha
InventorsShinji Kamihara, Kazuaki Kanai, Shigeru Noguchi
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Abstract
The present invention pertains to a process for the preparation of Compound (4) through the below-described reaction route: ##STR1## wherein R.sup.1 and R.sup.2 each represents H, halogen, OH or C.sub.1-6 alkyl group; X and Y each represents a protected amino group and n stands for 0 to 4. According to the above process, an aminotetralone derivative which is an intermediate useful for an industrial preparation of a camptothecin derivative can be obtained in a convenient manner and in a high yield.
Claims4
A process for the preparation of a compound represented by the following formula (2):
- ##STR6## wherein R.sup.1 and R.sup.2 each independently represents a hydrogen atom, a halogen atom, a hydroxyl group or a C.sub.1-6 alkyl group, X represents an amino group having a protective group and n stands for an integer of 0 to 4, which comprises, in the presence of a palladium catalyst, hydrogenating a compound represented by the following formula (1):
- ##STR7## wherein X, R.sup.1, R.sup.2 and n have the same meanings as defined above.
Dependencies are inferred from the claim text.