著者
沢田 誠吾 野方 健一郎 古田 富雄 横倉 輝男 宮坂 貞
出版者
公益社団法人日本薬学会
雑誌
Chemical & pharmaceutical bulletin (ISSN:00092363)
巻号頁・発行日
vol.39, no.10, pp.2574-2580, 1991-10-25

A radical substitution reaction of 20(S)-camptothecin (1) with methanol furnished 7-hydroxymethylcamptothecin (2). Reaction of 1 with primary alcohols higher than methanol gave 7-alkylcamptothecins (4), of which alkyl groups were one carbon less than the alcohols used and also 7-hydroxyalkylcamptothecins (5). For the preparation of 7-alkylcamptothecin (4), aldehydes were used as a radical source and several alkylated derivatives were synthesized. 7-Acyloxymethyl derivatives (6), 7-carbaldehyde (7), iminomethyl derivatives (10), acid (11), esters (12) and amides (13) were synthesized starting from 2. 7-Ethyl-(4b) and 7-propylcamptothecin (4c), acyloxymethyl compounds 6a, 6c and ethyl ester (12b) exhibited higher antitumor activity than 1 against L1210 in mice.

言及状況

Twitter (1 users, 1 posts, 0 favorites)

収集済み URL リスト