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2005
Other bioactive products
U 1300
Synthesis of Cribrostatin 6. — Cribrostatin 6 (XVIII), a growth inhibitor of cancer
and a number of pathogenic bacteria and fungi, is synthesized in ten steps from
11- 235 cells
phenol derivative (I) via the key intermediates (XII) and (XVII). Isoquinoline (XII) is
prepared according to the modified Pomeranz—Fritsch isoquinoline synthesis, and
preparation of amide (XVII) utilizes an intramolecular transfer reaction by catalytic
hydrogenation of 8-acyloxy-1-cyanoisoquinoline (XVI) to transfer an acetyl group
from oxygen to nitrogen. The final step employs air oxidation to form imidazo[5,1-a]isoquinolinedione (XVIII). — (NAKAHARA*, S.; KUBO, A.; Heterocycles 63 (2004) 10, 2355-2362; Meiji Pharm. Univ., Kiyose, Tokyo 204, Japan;
Eng.) — H. Hoennerscheid
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