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Double Dearomatization of Bis(diphenylphosphinamides) through Anionic Cyclization. A Facile Route of Accessing Multifunctional Systems with Antitumor Properties
文摘
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The sequentia
l one-pot doub
le dearomatization of bis(
N-benzy
l-
P,
P-dipheny
lphosphinamides) via anioniccyc
lization is described for the first time. Protonation and a
lky
lation of the dearomatized dianions providebis(tetrahydro-2,1-benzazaphospho
les) in good yie
ld and with very high regio- and stereocontro
l. Acid-cata
lyzed methano
lysis of the bisheterocyc
les affords bis(methy
l -aminophosphinates) stereospecifica
lly.The doub
ly phosphory
lated systems proved to be active against a series of cancer ce
ll lines.