- SYNTHESIS OF THE POTENT POTASSIUM CHANNEL OPENER Ro 31-6930 VIA CLAISEN REARRANGEMENT AND TANDEM REGIOCONTROLLED CYCLISATION.
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The synthesis of the potent potassium channel opener Ro 31-6930 is reported.Methods of controlling the regiochemistry of the crucial cyclisation are described.
- Attwood, Michael R.,Churcher, Ian,Dunsdon, Rachel M.,Hurst, David N.,Jones, Philip S.
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p. 811 - 814
(2007/10/02)
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- Benzopyran derivatives
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Compounds of the formula STR1 wherein R 1 is hydrogen, halogen, trifluoromethyl, nitro, cyano, lower alkyl, lower alkoxycarbonyl, lower alkylthio, lower alkylsulphonyl, lower alkanoyl, aroyl, carbamoyl, mono(lower alkyl)carbamoyl or di(lower alkyl)carbamoyl, R 2 is hydrogen, lower alkyl or phenyl, R 3 is hydrogen or lower alkyl, R 4 and R 5 each is hydrogen or R 4 is hydroxy and R 5 is hydrogen or R 4 and R 5 together are a carbon-carbon bond and R 6 is an aryl or N-heteroaryl group carrying a hydroxy group in the 2-position or, in the case of a N-heteroaryl group, also a N-oxide group in the 2-position, and pharmaceutically acceptable acid addition salts of these compounds of formula I which are basic, possess pronounced potassium channel activating activity and can be used as medicaments, particularly in the control or prevention of hypertension, congestive heart failure, angina pectoris, peripheral and cerebral vascular disease and smooth muscle disorders.
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