A short and efficient synthesis of 4-[2,2-dimethyl-4(tol-4-yl)benzochrom-3-en-7-yl]benzoic acid - a potent retinoic acid receptor antagonist.
An efficient synthesis of a potent RAR antagonist is described starting from disubstituted beta-naphthol. The functional groups on 2 and 3 positions of the beta-naphthol 5 were elaborated into benzochromanone 8. The title compound was prepared by Suzuki coupling of the left and right hand pieces.
Vuligonda
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Department of Chemistry, Allergan Inc, Irvine CA 92623, USA.
Chandraratna
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RA
D001565:Benzoates / Q000138:chemical synthesis*; D001578:Benzopyrans / Q000138:chemical synthesis*; D018168:Receptors, Retinoic Acid / Q000037:antagonists & inhibitors*
C121652:4-(2,2-dimethyl-4-(tol-4-yl)benzochrom-3-en-7-yl)benzoic acid; D001565:Benzoates; D001578:Benzopyrans; D018168:Receptors, Retinoic Acid